Home Transmembrane Transporters Calcium Channel inhibitor - P-gp inhibitor - P450 (e.g. CYP17) inhibitor Verapamil HCl For research use only.

Verapamil HCl

Synonyms: CP-16533-1, (±)-Verapamil

Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.

Verapamil HCl Chemical Structure

Verapamil HCl Chemical Structure

CAS: 152-11-4

Selleck's Verapamil HCl has been cited by 21 Publications

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Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116/VM46 cell Function assay 1 μM Effect on vinblastine IC50 against MDR human carcinoma HCT116/VM46 cell line at a dose of 1 uM concentration, IC50=0.004 μM 12729663
human MCF7/ADR cells Function assay 10 μM 48 h Inhibition of P-gp in human MCF7/ADR cells assessed as reversal of multidrug resistance at 10 uM by measuring EC50 for adriamycin-induced cytotoxicity after 48 hrs by SRB colorimetric assay, EC50=4.89 μM 25856545
NG108-15 Function assay The compound was tested for inhibition of calcium influx into neuronal (NG108-15) cells, IC50=6.5μM 2033584
CCRF-CEM Function assay The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin, ED50=0.045μM 7629817
CCRF-CEM Function assay The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM etoposide, ED50=3.4μM 7629817
MCF7/VP Function assay 20 uM 48 hrs Inhibition of MRP expressed in human MCF7/VP cells assessed as increase in vincristine-induced cytotoxicity at 20 uM after 48 hrs by SRB binding assay 8786364
MCF/ADR Function assay Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as increase in rhodamine 6G accumulation 8984151
B16/F10 Function assay Inhibition of human MDR1 expressed in mouse B16/F10 cells assessed as increase in doxorubicin accumulation by fluorimetry, ED50=3μM 9461658
HeLa Function assay TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells, Ki=2.9μM 9655880
K562/DOX MDR Cytotoxicity assay Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion, IC50=37μM 9986718
KBV1 Cytotoxicity assay 48 hrs Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method, IC50=1.6μM 10346948
KBV1 Cytotoxicity assay 48 hrs Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs by SRB method, IC50=39.2μM 10346948
KB31 Cytotoxicity assay 48 hrs Cytotoxicity against human KB31 cells after 48 hrs by SRB method, IC50=45.2μM 10346948
S1-B1-20 Function assay In vitro concentration required to inhibit tumor activity on subclone of human colon carcinoma cells (S1-B1-20) resistant to bisantrene, IC50=17.27μM 10377220
P388 Function assay Multidrug-resistant reversal activity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the presence of 10 nM vincristine, IC50=3.1μM 10386932
Caco-2 Function assay TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells, IC50=2.1μM 10820137
Caco-2 Function assay TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells, Ki=3μM 11405287
G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin efflux (Daunorubicin: ? uM) in G185 cells, IC50=4.2μM 11454724
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50=4.2μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=4.7μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50=6.5μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells, IC50=28.9μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells, IC50=38.2μM 11716514
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells, IC50=42μM 11716514
HCT15 Function assay 0.8 to 12.5 ug/mL Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL 11754602
UO31 Function assay 0.8 to 12.5 ug/mL Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL 11754602
CAKI1 Function assay 0.8 to 12.5 ug/mL Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL 11754602
MDA-435/LCC6 and MDA-435/LCC6-MDRI cells Function assay Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%, EC50=1.2μM 11784143
MDA-435/LCC6 and MDA-435/LCC6-MDRI cells Function assay Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%., EC50=2.4μM 11784143
MDA-435/LCC6 Function assay Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50=3.1μM 11784143
MDA435/LCC6 MDR1 Function assay TP_TRANSPORTER: reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells, EC50=3.1μM 11784143
MDA-435/LCC6 Function assay Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50=4.1μM 11784143
BTI-TN5B1-4 Function assay TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km=4.06μM 11785684
MDCK Function assay TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells, Ki=15.1μM 12134945
human embryonic kidney cells Function assay K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1, IC50=0.143μM 12190308
HCT15/CL02 Function assay TP_TRANSPORTER: drug resistance (paclitaxel) in HCT15/CL02 cells, IC50=2.21μM 12569305
MES-SA/DX5 Function assay TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells, IC50=4.78μM 12569305
Caco-2 Function assay TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells, Ki=0.88μM 12636153
L-MDR1 Function assay TP_TRANSPORTER: cell accumulation of calcein in L-MDR1 cells, IC50=18.9μM 12649369
LLC-PK1 Function assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=2μM 12699389
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells, IC50=2μM 12699389
LLC-PK1 Function assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=6.3μM 12699389
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells, IC50=6.3μM 12699389
LLC-PK1 Function assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=10μM 12699389
LLC-PK1 Function assay TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells, IC50=10μM 12699389
CHO Function assay Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1, IC50=0.143μM 12729675
mammalian cells Function assay Inhibition of human Potassium channel HERG expressed in mammalian cells, IC50=0.14125μM 12873512
AML-2/D100 Function assay TP_TRANSPORTER: drug resistance (vincristine) in AML-2/D100 cells, IC50=0.4μM 15240100
Caco-2 Function assay TP_TRANSPORTER: transepithelial transport of fexofenadine in Caco-2 cells, IC50=8.44μM 15359574
KB/MDR Function assay 1 h Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h, EC50=14μM 15481991
Sf9 Function assay Michaelis-Menten constant for human P-glycoprotein expressed in Sf9 cells, Km=2μM 15863325
K562 Function assay Reversal of P-gp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug concentration causing half-maximal increase in nuclear pirarubicin concentration, Activity=1.6μM 16279802
Caco-2 Function assay Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=20μM 17064079
MDA435/LCC6 Function assay Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, IC50=0.00025μM 17154505
MDA435/LCC6 Function assay Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, IC50=0.0052μM 17154505
MDA435/LCC6 Function assay Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, EC50=0.7μM 17154505
K562 Function assay Inhibition of human Pgp in anthracycline-resistant K562 cells assessed as drug level causing half maximal increase in nuclear concentration of pirarubicin, Activity=1.6μM 17256837
Caco-2 Antiproliferative assay 48 hrs Antiproliferative activity against human Caco-2 cells assessed as cell viability by MTT assay after 48 hrs, IC10=24.9μM 17276076
CEM/VLB500 Function assay 3 days Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay, EC50=1.041μM 17399990
A549 Function assay Inhibition of P-gp in A549 cells assessed as drug concentration required to double baseline fluorescence level by calcein-AM uptake assay, Activity=7μM 17419606
THP1 Antileishmanial assay Antileishmanial activity against wild-type Leishmania amazonensis MHOM/BR/1973/MM2269 promastigotes infected in human THP1 cells by luciferase based assay, IC50=19.1μM 17452480
THP1 Antileishmanial assay Antileishmanial activity against wild-type Leishmania major LV39 promastigotes infected in human THP1 cells by luciferase based assay, IC50=40.3μM 17452480
THP1 Antileishmanial assay Antileishmanial activity against wild-type Leishmania infantum MHOM/MA/67/ITMAP-263 promastigotes infected in human THP1 cells by luciferase based assay, IC50=43.2μM 17452480
KB-3-1 Cytotoxicity assay 5 uM 68 hrs Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay, IC50=0.0047μM 17488128
KB-C2 Cytotoxicity assay 5 uM 68 hrs Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-C2 cells at 5 uM after 68 hrs by MTT assay, IC50=0.1μM 17488128
BHK21 Cytotoxicity assay 10 to 20 uM Cytotoxicity against human MRP1 expressing hamster BHK21 cells at 10 to 20 uM by MTT assay 17646169
BHK21 Function assay Inhibition of human MRP1 mediated LTC4 transport in hamster BHK21 cells in presence of glutathione by rapid filtration technique 17646169
A2780/ADR Function assay Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50=4.57088μM 17890094
Caco-2 Function assay Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells, EC50=20μM 17936633
MDCK2 Function assay 10 uM 40 mins Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins 17964170
A2780 Function assay 30 mins Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay, IC50=4.57088μM 18083034
A2780 Function assay 30 mins Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50=6.60693μM 18083034
Caco-2 Function assay Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells, EC50=20μM 18257545
Caco-2 Function assay 100 uM Activation of human P-glycoprotein ATPase in Caco-2 cells assessed as ATP depletion at 100 uM 18257545
Caco-2 Function assay Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells, EC50=20μM 18276145
KBV20C Cytotoxicity assay Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of paclitaxel by MTS assay, IC50=0.01μM 18295490
KBV20C Cytotoxicity assay Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of vincristine by MTS assay, IC50=0.2μM 18295490
KBV20C Function assay Inhibition of Pgp in multidrug resistant human KBV20C cells assessed as increase in intracellular accumulation of Rh123 18295490
K562 Function assay Activity of Pgp-ATPase in doxorubicin-resistant human K562 cells, Km=0.7μM 18313307
K562 Function assay Inhibition of Verapamil-stimulated human Pgp-ATPase activity in doxorubicin-resistant K562 cells, Km=0.89μM 18313307
K562 Function assay Inhibition of Verapamil-stimulated human Pgp-ATPase activity in doxorubicin-resistant K562 cells, Vmax=22.39μM 18313307
K562 Function assay Activity of Pgp-ATPase in doxorubicin-resistant human K562 cells, Vmax=36.93μM 18313307
PC12 Autophagy assay 1 uM 24 hrs Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis 18391949
PC12 Autophagy assay 1 uM 96 hrs Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis 18391949
SK-N-MC Autophagy assay 1 uM 48 hrs Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis 18391949
SK-N-MC Autophagy assay 0.33 uM 24 hrs Induction of autophagy in human SK-N-MC cells assessed as increase in LC3-2 level at 0.33 uM after 24 hrs by immunoblotting analysis 18391949
SK-N-MC Autophagy assay 1 uM 48 hrs Induction of autophagy in Atg positive human SK-N-MC cells expressing EGFP-HDQ74 at 1 uM after 48 hrs 18391949
PC12 Autophagy assay 1 uM 24 hrs Induction of autophagy in pretreated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as calpain activation at 1 uM followed by doxycyline treatment measured after 24 hrs 18391949
SK-N-SH Autophagy assay 1 uM 48 hrs Induction of autophagy in human SK-N-SH cells expressing EGFP-HDQ74 assessed as inhibition of Bay K8644-induced EGFP-HDQ74 aggregation at 1 uM after 48 hrs 18391949
PC12 Autophagy assay 1 uM Induction of autophagy in differentiated rat stable inducible PC12 cells assessed as increase in LC3-2 level cell pretreated at 1 uM in presence of 400 nM bafilomycin A1 18391949
CHO Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.14125μM 18448342
RBMEC Function assay 10 umol/L 90 mins Inhibition of Pgp-mediated multidrug resistance activity in rat RBMEC cells assessed as Rh123 accumulation at 10 umol/L after 90 mins 18502125
Caco-2 Function assay Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells, EC50=20μM 18524592
A2780 Function assay Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=4.57088μM 18678495
A2780 Function assay Inhibition of P-gp in human A2780 cells, IC50=5.42μM 18707884
2008 Function assay Inhibition of human MRP1 in human 2008 cells, IC50=9.66μM 18707884
HEK293 Function assay Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy, IC50=6.8μM 18788725
MDCK2 Function assay 20 mins Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins, EC50=5.1μM 18849167
MCF7 Function assay Inhibition of human ERG in MCF7 cells, IC50=0.14454μM 19110341
K562 Function assay Reversal of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing maximum increase in nuclear concentration of pirarubicin by spectrofluorimetry relative to control, Alpha max=0.7μM 19140665
K562 Function assay Reversal of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing 50% increase in nuclear concentration of pirarubicin by spectrofluorimetry, Activity=1.6μM 19140665
K562 Function assay 1 uM 72 hrs Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 1 uM after 72 hrs by MTT assay 19140665
K562 Function assay 3 uM 72 hrs Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 3 uM after 72 hrs by MTT assay 19140665
smooth skeletal cells Function assay Displacement of (-)-[3H]devapamil from L-type calcium channel in rabbit smooth skeletal cells relative to verapamil, IC50=0.0602μM 19203272
A2780/ADR Function assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50=5.2μM 19250834
MDCK2 Function assay 20 mins Inhibition of human MDR1 expressed in MDCK2 cells assessed as enhancement of Calcein-AM uptake treated 30 mins before Calcein-AM challenge measured after 20 mins, IC50=14μM 19402665
BHK Function assay Induction of human histidine10-tagged MDR1 ATPase activity expressed in BHK cells by apparent Michaelis-Menten constant, Km=24μM 19402665
2008/MRP1 Function assay Reversal of MRP1-mediated doxorubicin-resistance in human 2008/MRP1 cells assessed as reduction of doxorubicin IC50 percent by half, Activity=2.6μM 19725578
2008/MRP1 Function assay Inhibition of MRP1 in human 2008/MRP1 cells by Lineweaver-Burke plot analysis, Ki=13.2μM 19725578
2008/MRP1 Function assay Inhibition of MRP1 in human 2008/MRP1 cells by dixon plot analysis, Ki=13.4μM 19725578
2008/MRP1 Function assay 120 mins Reversal of MRP1-mediated doxorubicin resistance in doxorubicin co-incubated human 2008/MRP1 cells assessed as minimum concentration required for restoration of doxorubicin accumulation after 120 mins by spectrofluorimetry relative to accumulation in huma 19725578
K562 Function assay Inhibition of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing 50% increase in nuclear concentration of pirarubicin by spectrofluorimetry, INH=1.6μM 20104851
MDCK Function assay 30 uM 1.5 hrs Inhibition of human MDR1 expressed in MDCK cells assessed as fluorescence activity at 30 uM after 1.5 hrs by rhodamine 123 efflux test 20363635
BHK21 Cytotoxicity assay 96 hrs Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay, IC50=10.6μM 20691599
K562 Function assay Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for maximum increase in nuclear concentration of pirarubicin by fluorescence assay, Alpha max=0.7μM 21145739
K562 Function assay Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for 50% increase in nuclear concentration of pirarubicin by fluorescence assay, IC50=1.6μM 21145739
HEK-293 Function assay Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA, IC50=41.5μM 21300721
HCT15 Function assay Inhibition of ABC transporter in human HCT15 cells assessed as calcein-AM efflux up to 100 uM 21348461
HCT15 Cytotoxicity assay Cytotoxicity against MDR1 expressing human HCT15 cells 21348461
HCT15 Function assay 40 uM Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 40 uM by fluorescence assay 21348461
A2780adr Function assay Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay, IC50=5.4μM 21354800
MDCK Function assay Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry, IC50=9.8μM 21354800
NIH-3T3 Function assay 10 uM 30 mins Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as daunomycin efflux at 10 uM after 30 mins by flow cytometry 21856049
MDCK Function assay 30 mins Inhibition of human MDR1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay, IC50=0.5μM 22112208
MDCK Function assay 30 mins Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay, IC50=6.8μM 22112208
Caco2 Function assay 5 to 25 uM 1.5 hrs Inhibition of P-glycoprotein overexpressed in human Caco2 cells assessed as increase in digoxin accumulation at 5 to 25 uM incubated for 1.5 hrs prior to digoxin treatment measured after 1.5 hrs by LC/MS/MS analysis 22209486
LCC6MDR Function assay 5 days Reversal of P-gp-mediated doxorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.245μM 22320402
LCC6MDR Function assay 5 days Reversal of P-gp-mediated vincristine-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.385μM 22320402
LCC6MDR Function assay 5 days Reversal of P-gp-mediated paclitaxel-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.428μM 22320402
LCC6MDR Function assay 5 days Reversal of P-gp-mediated vinblastin-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.503μM 22320402
MDA435/LCC6MDR Function assay Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Lineweaver-Burk plot analysis, Ki=1.75μM 22320402
MDA435/LCC6MDR Function assay Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Dixon plot analysis, Ki=1.75μM 22320402
MDA435/LCC6MDR Function assay 150 mins Inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin after 150 mins by fluorescence spectrophotometric analysis, MIC=8μM 22320402
K562/A02 Function assay 10 uM Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated 24 hrs before adriamycin challenge followed by drug washout by MTS assay, IC50=12.92μM 22405646
K562/A02 Function assay 10 uM 24 hrs Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated for 24 hrs followed by adriamycin treated 6 hrs after drug washout by MTS assay, IC50=26.06μM 22405646
K562/A02 Function assay 0.25 to 5 after 60 mins Inhibition of p-glycoprotein-mediated rhodamine 123 efflux in human K562/A02 cells at 0.25 to 5 after 60 mins by fluorescence microscopic analysis 22405646
K562/A02 Function assay 10 uM 30 mins Inhibition of Pgp-mediated rhodamine 123 efflux in human K562/A02 cells assessed as intracellular rhodamine 123 accumulation at 10 uM preincubated for 30 mins measured after 60 mins by fluorescence microscopy relative to control 22429509
K562/A02 Function assay 10 uM 24 hrs Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout before addition of adriamycin measured after 72 hrs by MTS assay (Rvb = 33.59 uM) 22429509
K562/A02 Function assay 10 uM 24 hrs Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 6 hrs post washout measured after 72 hrs by MTS assay (Rvb = 35 22429509
K562/A02 Function assay 10 uM 24 hrs Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 12 hrs post washout measured after 72 hrs by MTS assay (Rvb = 5 22429509
K562/A02 Function assay 10 uM 24 hrs Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 24 hrs post washout measured after 72 hrs by MTS assay (Rvb = 5 22429509
K562/A02 Function assay 0.33 to 10 uM 60 mins Inhibition of Pgp-mediated rhodamine-123 efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of rhodamine-123 at 0.33 to 10 uM after 60 mins by flow cytometry analysis 22450134
K562/A02 Function assay 0.33 to 10 uM 60 mins Inhibition of Pgp-mediated rhodamine-123 efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of rhodamine-123 at 0.33 to 10 uM after 60 mins by fluorescence microscopic analysis 22450134
K562/A02 Function assay 0.33 to 10 uM 60 mins Inhibition of Pgp-mediated adriamycin efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of adriamycin at 0.33 to 10 uM after 60 mins by FACS flow cytometry 22450134
CCRF-CEM/VCR1000 Function assay 240 secs Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50=0.57544μM 22452412
BHK Function assay 30 mins Induction of ATPase activity of human His10-tagged P-gp expressed in BHK cells assessed as inorganic phosphate release after 30 mins by Michaelis-Menten analysis, Km=24μM 22533905
HEK293 Function assay Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=32μM 22587986
KBVIN Function assay 10 uM 72 hrs Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as paclitaxel-induced cytotoxicity at 10 uM after 72 hrs by SRB assay 22612652
KBVIN Function assay 10 uM 72 hrs Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as vincristine-induced cytotoxicity at 10 uM after 72 hrs by SRB assay 22612652
KBVIN Function assay 10 uM 72 hrs Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as doxorubicin-induced cytotoxicity at 10 uM after 72 hrs by SRB assay 22612652
C1-6-37-3 Function assay 30 mins Inhibition of human voltage-dependent L-type calcium channel subunit alpha1C/alpha2delta/beta2a expressed in C1-6-37-3 cells assessed as inhibition of K+-induced calcium influx incubated for 30 mins prior to K+-induction by Fluo-4-AM based FLIPR assay, IC50=0.9μM 22694270
BHK Function assay Binding affinity to human His10-tagged P-gp expressed in BHK cells assessed as induction of ATPase activity measured as inorganic phosphate release by spectrophotometric analysis, Km=24μM 22727780
ovary cells Function assay Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit, IC50=23.5μM 22761000
embryonic kidney cells Function assay Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit, IC50=24μM 22761000
embryonic kidney cells Function assay Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit, IC50=47μM 22761000
L929 Function assay Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method, IC50=8μM 23084278
K562 Function assay Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as half maximal increase of pirarubicin accumulation by spectrofluorometric analysis, IC50=1.6μM 23245571
KB/VCR Function assay 72 hrs Inhibition of p-gp in human KB/VCR cells assessed as potentiation of 100 nM docetaxel-induced cytotoxicity after 72 hrs by MTT assay, EC50=1.253μM 23683834
KB/VCR Function assay 5 uM 72 hrs Inhibition of p-gp in human KB/VCR cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM after 72 hrs by MTT assay 23683834
KB/VCR Function assay 5 uM 72 hrs Inhibition of p-gp in human KB/VCR cells assessed as potentiation of vincristine-induced cytotoxicity at 5 uM after 72 hrs by MTT assay 23683834
CHO Function assay Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50=0.2μM 23812503
MDA435/LCC6MDR Function assay Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50=0.4457μM 24171478
MDCK Function assay 30 mins Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay, EC50=20μM 24607999
MDCK Function assay 100 uM 2 hrs Activation of ATPase activity of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction of reduction of ATP level at 100 uM after 2 hrs by luminescence/ATPlite assay 24607999
NCI/ADR-RES Function assay 20 mins Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay 24992153
MDCK Function assay 30 mins Inhibition of MRP1 (unknown origin) expressed in MDCK cells after 30 mins by Calcein-AM assay, IC50=3.5μM 25093931
NCI-H292 Cytotoxicity assay 50 uM 72 hrs Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=0.18μM 25215856
NCI-H292 Cytotoxicity assay 50 uM 72 hrs Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=1.2μM 25215856
H460 Cytotoxicity assay 50 uM 72 hrs Potentiation of erlotinib-induced cytotoxicity against human H460 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=10.3μM 25215856
H460/Vbl Cytotoxicity assay 50 uM 72 hrs Potentiation of erlotinib-induced cytotoxicity against human H460/Vbl cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=13.3μM 25215856
H460 Cytotoxicity assay 50 uM 72 hrs Potentiation of gefitinib-induced cytotoxicity against human H460 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=19.6μM 25215856
H460/Vbl Cytotoxicity assay 50 uM 72 hrs Potentiation of gefitinib-induced cytotoxicity against human H460/Vbl cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=25.7μM 25215856
K562 Function assay 3 uM 72 hrs Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562 cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.023 +/- 0.004 uM), IC50=0.029μM 25282263
K562/DOX Function assay 3 uM 72 hrs Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562/DOX cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 2.00 +/- 0.24 uM), IC50=0.74μM 25282263
K562/DOX Function assay Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay, IC50=1.6μM 25282263
A7R5 Function assay 15 mins Antagonist activity at calcium channel in rat A7R5 cells assessed as inhibition of Cacl2/KCl-induced increase in intracellular Ca2+ incubated for 15 mins prior to Cacl2/KCl challenge by fluorescence assay, IC50=0.3μM 25311564
MES-SA Function assay 15 mins Modulation of P-gp mediated drug efflux in human MES-SA cells assessed as accumulation of rhodamine-123 incubated for 15 mins prior to rhodamine-123 addition measured after 1 hr by fluorescence analysis, EC50=7.1μM 25311564
H69 Function assay 15 mins Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis, EC50=27.8μM 25311564
MES-SA Function assay 15 mins Modulation of BCRP1 mediated drug efflux in mitoxantrone-resistant human MES-SA cells assessed as accumulation of hoechst 33342 incubated for 15 mins prior to rhodamine-123 addition measured after 90 mins by fluorescence analysis, EC50=37.3μM 25311564
K562/ADR Function assay 10 uM 2.5 hrs Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence microscopy 25462264
K562/ADR Function assay 10 uM 2.5 hrs Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence spectrophotometry 25462264
K562/ADR Cytotoxicity assay 10 uM 48 hrs Potentiation of adriamycin-induced cytotoxicity against human K562/ADR cells at 10 uM after 48 hrs by MTT assay 25462264
K562/A02 Function assay 5 uM 48 hrs Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM after 48 hrs by MTT assay, IC50=6.8μM 25464884
K562/A02 Function assay 5 uM 24 hrs Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs prior to adriamycin treatment measured after 48 hrs by MTT assay, IC50=9.6μM 25464884
K562/A02 Function assay 2.5 uM 48 hrs Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay, IC50=15.92μM 25464884
K562/A02 Function assay 5 uM 24 hrs Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs followed by adriamycin treatment post compound washout measured after 48 hrs by MTT assay, IC50=40.8μM 25464884
KB/VCR Cytotoxicity assay 25 uM 72 hrs Cytotoxicity against human KB/VCR cells assessed as vincristine IC50 at 25 uM after 72 hrs by SRB method, IC50=0.02μM 25597010
K562/R7 Cytotoxicity assay 1 uM 72 hrs Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.6μM 25634041
MDA435/LCC6MDR Function assay 1 uM 5 days Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 1 uM after 5 days by CellTiter 96 Aqueous assay, IC50=0.038μM 25985195
MDA435/LCC6MDR Function assay 5 days Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing doxorubicin resistance measured as cell survival after 5 days by MTS assay, EC50=0.245μM 25985195
MDA435/LCC6MDR Function assay 5 days Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing vincristine resistance measured as cell survival after 5 days by MTS assay, EC50=0.385μM 25985195
MDA435/LCC6MDR Function assay 5 days Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay, EC50=0.446μM 25985195
MDA435/LCC6MDR Function assay 5 days Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing vinblastine resistance measured as cell survival after 5 days by MTS assay, EC50=0.503μM 25985195
MDA435/LCC6MDR Function assay 3 uM 150 mins Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as restoration of intracellular doxorubicin accumulation at 3 uM after 150 mins by spectrofluorometric analysis relative to parental cells 25985195
MDA435/LCC6MDR Function assay Modulation of P-gp in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50=0.446μM 26233798
KB/VJ300 Cytotoxicity assay 72 hrs Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay in presence of 0.121 uM vincristine, IC50=10.3μM 26717050
NIH/3T3 Cytotoxicity assay Intrinsic cytotoxicity against mouse NIH/3T3 cells by MTT assay, CC50=27μM 26836364
MCF7/D70 Function assay 10 uM 72 hrs Inhibition of P-gp in human MCF7/D70 cells assessed as decrease in doxorubicin IC50 at 10 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.906 +/- 0.02 uM), IC50=0.2μM 26840362
A549/CDDP Function assay 1.2 uM Inhibition of P-gp in human A549/CDDP cells assessed as accumulation of rhodamine 123 at 1.2 uM by flow cytometry 26891099
KB/VJ300 Growth inhibition assay 72 hrs Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay, IC50=4.6μM 26918761
K562/A02 Function assay 5 uM 48 hrs Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM), IC50=8.5μM 27073052
K562/A02 Function assay 2.5 uM 48 hrs Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM), IC50=19.84μM 27073052
L5178Y Cytotoxicity assay 72 hrs Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=47.85μM 27156771
HLF Cytotoxicity assay 48 hrs Cytotoxicity against HLF cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=27.18μM 27328029
MDA435/LCC6MDR Function assay 1 uM 5 days Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM), IC50=0.0351μM 27750197
MDA435/LCC6MDR Function assay 5 days Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of doxorubicin cytotoxic IC50 by half after 5 days by Cell Titer 96 Aqueous assay, EC50=0.245μM 27750197
MDA435/LCC6MDR Function assay 150 mins Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in doxorubicin accumulation to half of parental LCC6 cells measured after 150 mins by fluorescence spectrophotometric method, EC50=0.35μM 27750197
MDA435/LCC6MDR Function assay 5 days Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vincristine cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay, EC50=0.385μM 27750197
MDA435/LCC6MDR Function assay 5 days Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of paclitaxel cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay, EC50=0.446μM 27750197
MDA435/LCC6MDR Function assay 5 days Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vinblastine cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay, EC50=0.503μM 27750197
K562 Function assay 10 uM 1 hr Inhibition of P-gp in doxorubicin resistant human K562 cells assessed as increase in accumulation of rhodamine 123 at 10 uM measured after 1 hr by flow cytometry 27908756
MES-SA/Dx5 Function assay 72 hrs Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring compound concentration required for reduction of doxorubicin IC50 by half after 72 hrs by MTT assay, EC50=0.7μM 28043777
MES-SA/Dx5 Function assay 72 hrs Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring compound concentration required for reduction of paclitaxel IC50 by half after 72 hrs by MTT assay, EC50=0.8μM 28043777
MES-SA/Dx5 Function assay 72 hrs Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of actinomycin D-induced cytotoxicity by measuring compound concentration required for reduction of actinomycin D IC50 by half after 72 hrs by MTT assay, EC50=0.9μM 28043777
MES-SA/Dx5 Function assay 72 hrs Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of vinblastine-induced cytotoxicity by measuring compound concentration required for reduction of vinblastine IC50 by half after 72 hrs by MTT assay, EC50=1μM 28043777
K562/A02 Function assay 0.33 to 10 uM 1 hr Inhibition of P-gp in human K562/A02 cells assessed as increase in intracellular rhodamine123 accumulation at 0.33 to 10 uM measured after 1 hr by flow cytometry 28068095
LoVo/DX Function assay 2.5 to 10 uM 15 mins Inhibition of P-gp in human LoVo/DX cells assessed as reduction in Rhodamine123 efflux at 2.5 to 10 uM preincubated for 15 mins followed by Rhodamine123 addition measured after 1 hr by flow cytometry 28109950
LoVo/DX Function assay 10 uM 2 hrs Substrate activity at P-gp in human LoVo/DX cells assessed as ATP consumption at 10 uM after 2 hrs by ATPlite assay 28109950
K562/DOX Function assay 30 mins Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by spectroflurometry, I0.5=1.6μM 28113128
MCF7/DX Function assay 5 uM 48 hrs Reversal of multidrug resistance in human MCF7/DX cells assessed as potentiation doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 level at 5 uM incubated for 48 hrs by MTT assay, IC50=6.59μM 28245113
K562/A02 Cytotoxicity assay 48 hrs Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay, IC50=31.28μM 28301155
K562 Cytotoxicity assay 48 hrs Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=36.7μM 28301155
K562/A02 Function assay 5 uM 2.5 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular adriamycin accumulation at 5 uM after 2.5 hrs by spectrofluorimetric analysis 28301155
K562/A02 Function assay 5 uM up to 90 mins Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular Rh123 accumulation at 5 uM up to 90 mins by flow cytometry 28301155
K562/A02 Function assay 5.0 uM up to 90 mins Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as intracellular Rh123 accumulation at 5.0 uM measure up to 90 mins by flow cytometric analysis 28355069
K562/A02 Function assay 5 uM 24 hrs Inhibition of P-gp in human K562/A02 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 5 uM preincubated for 24 hrs followed by doxorubicin addition measured after 48 hrs by MTT assay 28355069
K562/A02 Function assay 5.0 uM 150 mins Inhibition of P-gp in human K562/A02 cells assessed as accumulation of doxorubicin at 5.0 uM after 150 mins by fluorescence spectrophotometric analysis 28355069
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=10.73μM 28645831
K562/A02 Function assay 5 uM 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM), IC50=17.55μM 28645831
K562/A02 Function assay 48 hrs Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=31.28μM 28645831
K562/A02 Function assay 0.5 to 2.5 uM 60 mins Inhibition of ABCB1 in human K562/A02 cells assessed as increase in adriamycin accumulation at 0.5 to 2.5 uM pretreated for 60 mins followed by ADR addition after 90 mins by fluorescence spectrophotometric method 28645831
CHO Function assay Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method, IC50=0.53μM 28797771
SW620/AD300 Function assay 2 uM 30 to 120 mins Inhibition of ABCB1 in human SW620/AD300 cells assessed as reduction in Rh123 efflux at 2 uM treated followed by Rh123 addition in Rh123 free medium for 30 to 120 mins by flow cytometry 29126726
K562/Dox Function assay Inhibition of P-gp in human K562/Dox cells assessed as increase in nuclear accumulation of pirarubicin by spectrofluorometric assay, IC50=1.6μM 29162309
MCF7/ADR Function assay 48 hrs Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity after 48 hrs by MTT assay, EC50=0.2451μM 29407947
MCF7/ADR Function assay 150 mins Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Lineweaver-Burk plot analysis, Ki=2.88μM 29407947
MCF7/ADR Function assay 150 mins Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Dixon plot analysis, Ki=2.92μM 29407947
MCF7/ADR Function assay 150 mins Inhibition of P-gp in human MCF7/ADR cells assessed as concentration required to restore doxorubicin accumulation in cells after 150 mins by fluorescence assay relative to MCF7 cells, Activity=40μM 29407947
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=48.91μM 29407947
MCF7/ADR Function assay 10 uM 4 hrs Inhibition of P-gp mediated efflux in human MCF7/ADR cells at 10 uM after 4 hrs by Rh123 dye-based flow cytometric method 29407947
K562/Dox Function assay Inhibition of P-gp in human K562/Dox cells assessed as compound concentration causing 50% increase in nuclear accumulation of pirarubicin by spectrofluorometric method, Activity=1.6μM 29421572
K562/A02 Function assay 5 uM 2.5 hrs Inhibition of P-gp in human K562/A02 cells assessed as increase in adriamycin accumulation at 5 uM after 2.5 hrs by flow cytometry method 29631786
K562 Function assay 5 uM 2.5 hrs Inhibition of P-gp in human K562 cells assessed as increase in Rh123 accumulation at 5 uM after 2.5 hrs by by flow cytometry method 29631786
MCF7/ADR Function assay 48 hrs Inhibition of P-gp in human MCF7/ADR cells assessed as cell viability after 48 hrs by MTT assay, EC50=20.54μM 29656198
KB/VJ300 Growth inhibition assay 72 hrs Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of 0.1 uM of vincristine by MTT assay, IC50=0.1μM 29746134
MCF7/ADR Function assay 10 uM 2 hrs Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular Rh123 accumulation at 10 uM after 2 hrs by flow cytometry 29903663
SW620/AD300 Function assay 2 hrs Inhibition of ABCB1 in human SW620/AD300 cells assessed as intracellular accumulation of paclitaxel up to 2 uM treated at 2 hrs post paclitaxel treatment for 30 mins in paclitaxel free medium by HPLC analysis 29975529
SW620/AD300 Function assay 4 hrs Inhibition of ABCB1 in human SW620/AD300 cells assessed as decrease in rhodamine 123 efflux up to 2 uM preincubated for 4 hrs followed by 30 mins incubation in Rho-123 containing medium and subsequent incubation in Rho-123 free medium up to 120 mins by fl 29975529
SW620/AD300 Function assay 4 hrs Inhibition of ABCB1 in human SW620/AD300 cells assessed as intracellular accumulation of [3H]-paclitaxel up to 2 uM preincubated for 4 hrs followed by [3H]-paclitaxel addition measured after 2 hrs by liquid scintillation counting method 29975529
MCF7 Cytotoxicity assay 10 ug/ml 48 hrs Potentiation of adriamycin-induced cytotoxicity in human MCF7 cells assessed as adriamycin IC50 at 10 ug/ml after 48 hrs by MTT assay (Rvb = 1.3 +/- 0.2 uM), IC50=1.5μM 30137985
MCF7/ADR Function assay 10 ug/ml 24 hrs Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular accumulation of adriamycin by measuring increase in fluorescence intensity at 10 ug/ml after 24 hrs by fluorescence microscopic analysis 30137985
KBV Function assay 10 uM 72 hrs Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 1353.98 +/- 303.33 nM), IC50=0.02816μM 30347326
KBV Function assay 10 uM 2 hrs Inhibition of P-gp-mediated Rh-123 efflux in human KBV cells assessed as Rh-123 accumulation at 10 uM preincubated for 2 hrs followed by Rh-123 addition measured after 30 mins by flow cytometry 30347326
2008/MRP1 Function assay 5 days Inhibition of MRP1 in human 2008/MRP1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reduction in cell survival after 5 days by MTS assay, EC50=1.925μM 30351934
KBV Function assay 10 uM Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM, IC50=0.0049μM 30384042
KBV Function assay 10 uM 72 hrs Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=6.15μM 30384042
MDCK Function assay 30 mins Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method, IC50=1.3μM 30384046
MDCK Function assay 30 mins Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method, IC50=4.5μM 30384046
KBV Cytotoxicity assay 10 uM 48 hrs Potentiation of vincristine-induced cytotoxicity against human KBV cells assessed as vincristine IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 666.3 nM), IC50=0.00131μM 30455148
A2780/TAX Cytotoxicity assay 10 uM 48 hrs Potentiation of paclitaxel-induced cytotoxicity against human A2780/TAX cells assessed as paclitaxel IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 3970 nM), IC50=0.0188μM 30455148
A2780/CDDP Cytotoxicity assay 10 uM 48 hrs Potentiation of cisplatin-induced cytotoxicity against human A2780/CDDP cells assessed as cisplatin IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 43.11 nM), IC50=0.04011μM 30455148
Lucena 1 Function assay 12.5 uM 1 hr Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 12.5 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry 30613324
Lucena 1 Function assay 25 uM 1 hr Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 25 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry 30613324
MCF7/ADR Antiproliferative assay 5 uM 48 hrs Potentiation of adriamycin-induced antiproliferative activity against human MCF7/ADR cells assessed as adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 89.14 +/- 4.89 uM), IC50=2.25μM 30837097
MCF7/ADR Function assay 48 hrs Inhibition of P-gp in doxorubicin-resistant human MCF7/ADR cells assessed as reversal of doxorubicin resistance by measuring doxorubicin IC50 incubated for 48 hrs by MTT assay (Rvb = doxorubicin alone = 64.8 +/- 2.1 uM), IC50=4.7μM 30860373
KB/VJ300 Cytotoxicity assay 72 hrs Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay, IC50=0.8μM 30869890
MCF7/Dox Function assay 12.5 uM 48 hrs Reversal of P-gp-mediated multidrug resistance in human MCF7/Dox cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 12.5 uM after 48 hrs by MTT assay (Rvb = 51.19 +/- 0.95 microM), IC50=10.1μM 31325783
KBtax Function assay 100 uM 1 hr Inhibition of P-gp efflux in human KBtax cells at 100 uM after 1 hr by flow cytometry 31419740
MDCK-MDR1 Function assay 30 mins Inhibition of P-gp (unknown origin) expressed in MDCK-MDR1 cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay, EC50=0.5μM 31494468
MDCK Function assay 30 mins Inhibition of BCRP (unknown origin) expressed in MDCK cells assessed as increase in Hoechst 33342 accumulation incubated for 30 mins by Hoechst 33342 dye based fluorescence assay, EC50=0.9μM 31494468
K562/DOX Function assay 30 mins Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by fluorescence based assay, I0.5=1.6μM 31494468
MDCK Function assay 30 mins Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay, EC50=6.8μM 31494468
KBV Function assay 10 uM 72 hrs Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 352.31 +/- 10.9 nM), IC50=0.01843μM 31505451
KBV Function assay 10 uM 72 hrs Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 2.92 +/- 0.31 nM), IC50=0.03502μM 31505451
KBV Function assay 10 uM 72 hrs Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of irinotecan-induced cytotoxicity by measuring irinotecan IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 49.2 +/- 0.46 nM), IC50=10.37μM 31505451
12D7-MDR Function assay Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate, IC50=1.2μM 31505928
HepG2/DOX Function assay 10 uM Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay (Rvb = 69.3 +/- 3.9 uM), IC50=1.3μM 31585275
MCF7/ADM Function assay 10 uM Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay (Rvb = 151.7 +/- 5 uM), IC50=3.7μM 31585275
HepG2/DOX Function assay 5 uM Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay (Rvb = 69.3 +/- 3.9 uM), IC50=4.7μM 31585275
MCF7/ADM Function assay 5 uM Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay (Rvb = 151.7 +/- 5 uM), IC50=17.8μM 31585275
HepG2/Dox Function assay 10 uM 4 hrs Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular doxorubicin accumulation at 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by fluorescence microscopic analy 31585275
HepG2/Dox Function assay 10 uM 4 hrs Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by fluorescence microscopic analysis 31585275
HepG2/Dox Function assay 5 to 10 uM 4 hrs Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular doxorubicin accumulation at 5 to 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by flow cytometry analysis 31585275
HepG2/Dox Function assay 5 to 10 uM 4 hrs Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular Rhodamine123 accumulation at 5 to 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by flow cytometry analysis 31585275
MCF7/ADM Function assay 10 uM 4 hrs Reversal of P-gp mediated drug efflux in human MCF7/ADM cells assessed as increase in intracellular doxorubicin accumulation at 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by fluorescence microscopic analys 31585275
MCF7/ADM Function assay 10 uM 4 hrs Reversal of P-gp mediated drug efflux in human MCF7/ADM cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by fluorescence microscopic analysis 31585275
HepG2/Dox Function assay 5 to 10 uM 4 hrs Inhibition of P-gp mediated doxorubicin efflux in human HepG2/Dox cells at 5 to 10 uM preincubated for 4 hrs followed by co-incubation with doxorubicin for 2 hrs followed by doxorubicin wash-out and measured after 120 mins incubation with drug containing 31585275
MCF7/ADM Function assay 5 to 10 uM 4 hrs Inhibition of P-gp mediated doxorubicin efflux in human MCF7/ADM cells at 5 to 10 uM preincubated for 4 hrs followed by co-incubation with doxorubicin for 2 hrs followed by doxorubicin wash-out and measured after 120 mins incubation with drug containing c 31585275
KB/VJ300 Antiproliferative assay 72 hrs Antiproliferative activity against human vincristine-rsistant KB/VJ300 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50=0.4μM 31642315
CHO Cytotoxicity assay Cytotoxicity against CHO cells by MTT assay, IC50=0.56μM ChEMBL
CHRC5 Function assay Tested for in vitro proliferation and viability of multidrug resistant CHRC5 Chinese hamster cells in the presence and absence of doxorubicin in a modified MTT assay, EC50=1.2μM ChEMBL
HeLa Function assay 30 mins Inhibition of P-glycoprotein 1 in human HeLa cells assessed as intracellular accumulation of Hoechst 33342 dye after 30 mins by fluorescence microscopic analysis, IC50=1.7μM ChEMBL
HEK293 Function assay 24 hrs Inhibition of Marburg virus envelope glycoprotein-mediated cell entry in rVSIV-deltaG-MarV-GP pseuotype virus infected HEK293 cells after 24 hrs post transfection by luciferase reporter gene assay, IC50=13μM ChEMBL
K562/ADR Function assay 10 to 20 uM 30 mins Inhibition of P-glycoprotein in human K562/ADR cells at 10 to 20 uM after 30 mins by rhodamine 123 staining-based fluorescence assay ChEMBL
K562 Function assay 10 to 20 uM 1 hr Inhibition of P-glycoprotein in doxorubicin-resistant Homo sapiens (human) K562 cells overexpressing P-gp assessed as increase in intracellular Rh123 accumulation at 10 to 20 uM after 1 hr by flow cytometric analysis ChEMBL
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Biological Activity

Description Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
Targets
Calcium channel [2]
In vitro
In vitro

The enzyme hydrolase activity of recombinant CES2 is substantially inhibited by diltiazem and verapamil (Ki = 0.25 ± 0.02 and 3.84 ± 0.99μM, respectively).
In Vivo
In vivo

Verapamil confers an anti-arrhythmic effect via calcium influx inhibition, inhibition of oxygen consumption and accompanied by preservation of Cx43 protein in rat heart.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05618132 Recruiting Angina Pectoris Variant|Angina Pectoris; Spasm-Induced|Angina Pectoris With Normal Coronary Arteriogram University Hospital Antwerp January 9 2023 Not Applicable
NCT04406259 Recruiting Cluster Headache Centre Hospitalier Universitaire de Nice November 2 2020 Phase 4
NCT04014634 Unknown status Cluster Headache Episodic|Greater Occipital Nerve Injection Leiden University Medical Center|Netherlands Brain Foundation|Innovatiefonds Zorgverzekeraars August 1 2019 Phase 4

Chemical lnformation & Solubility

Molecular Weight 491.06 Formula

C27H38N2O4.HCl
CAS No. 152-11-4 SDF Download Verapamil HCl SDF
Smiles CC(C)C(CCCN(C)CCC1=CC(=C(C=C1)OC)OC)(C#N)C2=CC(=C(C=C2)OC)OC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 98 mg/mL ( (199.56 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : 12 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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