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Calcitriol

Name: Calcitriol
Brand: Selleck Chemicals
SKU: S1466
Rating: 5 (51 reviews)

Synonyms: RO215535, Topitriol, 1,25-Dihydroxyvitamin D3

Catalog No.S1466 Purity: 99.96%

Calcitriol is a nonselective vitamin D receptor activator/agonist(VDRA), exhibiting a 10-fold higher vitamin D receptor (VDR) binding affinity(IC50=0.4 nM) than the selective VDRA paricalcitol. Solutions are unstable and should be fresh-prepared.

Calcitriol Chemical Structure

CAS: 32222-06-3

Selleck's Calcitriol has been cited by 51 publications

Purity & Quality Control

Batch: Purity: 99.96%

99.96

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human HCT116	Cytotoxic assay		120 h	Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs, IC50=1e-05 μM	22926068
HOS	Function assay			Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay, EC50 = 0.00001 μM.	21889334
SK-MEL-188	Growth inhibition assay		48 hrs	Growth inhibition of human SK-MEL-188 cells measured after 48 hrs by MTS/PMS assay, IC50 = 0.00001 μM.	27070779
osteosarcoma cells	Function assay			Effect on VDR transcriptional activity in human osteosarcoma cells, EC50 = 0.0000106 μM.	18054230
HOS/SF	Function assay		24 hrs	Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.000026 μM.	24900728
LM05e	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse LM05e cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.00003 μM.	24900339
HEK293	Function assay			Transrepression of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-NCoR and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in NCoR recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay, IC50 = 0.00005 μM.	29989817
HEK293	Function assay			Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-RXRalpha and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in interaction with RXRalpha by beta-galactosidase reporter gene based mammalian two-, EC50 = 0.00007 μM.	29989817
HEK293T	Function assay			Agonist activity at GAL4 DNA-binding domain fused VDR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.0000953 μM.	30144697
HEK293	Function assay			Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay, IC50 = 0.0001 μM.	26613420
HEK293	Function assay		16 to 24 hrs	Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay, EC50 = 0.00012 μM.	26613420
ROS 17/2.8	Function assay		16 hrs	Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay, EC50 = 0.0002 μM.	19167893
osteosarcoma cells	Function assay			Activity at VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcription by reporter gene assay, EC50 = 0.0002 μM.	17960924
ROS 17/2.8	Function assay		16 hrs	Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay, EC50 = 0.0002 μM.	18722130
ROS 17/2.8	Function assay		16 hrs	Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay, Ki = 0.0002 μM.	21105677
ROS 17/2.8	Function assay		16 hrs	Agonist activity at rat VDR in ROS 17/2.8 cells transfected with Cyp24a1 reporter plasmid assessed as increase in Cyp24a1 transcription after 16 hrs by luciferase reporter gene assay, EC50 = 0.0002 μM.	22018918
osteosarcoma cells	Function assay			Induction of VDR-mediated 24-hydroxylase transcription in rat osteosarcoma cells by luciferase reporter gene assay, ED50 = 0.0002 μM.	21902235
osteosarcoma cells	Function assay			Transactivation of VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcriptional activity by luciferase reporter gene assay, ED50 = 0.0002 μM.	26630444
osteosarcoma cells	Function assay		16 hrs	Inhibition of VDR-induced 24-hydroxylase transcription in rat osteosarcoma cells after 16 hrs by luciferase reporter gene assay, ED50 = 0.0002 μM.	22490010
osteosarcoma cells	Function assay			Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assay, EC50 = 0.0003 μM.	19819702
HuH7	Function assay		24 hrs	Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay, EC50 = 0.0003 μM.	27145071
ROS 17/2.8	Function assay			Vitamin D3 receptor-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells, ED50 = 0.00035 μM.	10479276
ROS 17/2.8	Function assay			In vitro vitamin D receptor (VDR)-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells, ED50 = 0.00036 μM.	11000014
ROS 17/2.8	Function assay			In vitro vitamin D receptor-mediated antiproliferative activity in rat osteosarcoma ROS 17/2.8 cells, ED50 = 0.0004 μM.	11931627
COS7	Function assay			Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay, EC50 = 0.0005 μM.	17298045
COS7	Function assay		24 hrs	Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50 = 0.0005 μM.	17904370
SVEC	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse SVEC cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.00052 μM.	24900339
osteosarcoma cells	Function assay			Effect on VDR transcriptional activity in human osteosarcoma cells in presence of 5% fetal calf serum, EC50 = 0.000555 μM.	18054230
HEK293	Function assay			Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay, EC50 = 0.0006 μM.	26613420
CV1	Function assay			Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells, ED50 = 0.0007 μM.	17149880
NHEK	Antiproliferative assay		24 hrs	Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay, EC50 = 0.000728 μM.	22404326
COS1	Function assay			Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells, IC50 = 0.0008 μM.	17924616
HEK293	Function assay		24 hrs	Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50 = 0.001 μM.	17904370
HL60	Function assay			Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium, ED50 = 0.001 μM.	21902235
HeLa	Function assay		16 hrs	Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay, EC50 = 0.001 μM.	22957834
T47D	Antiproliferative assay		72 hrs	Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.0013 μM.	24900339
ROS 17/2.8	Function assay			Activity at human recombinant VDR in ROS 17/2.8 cells transfected with growth hormone fusion gene VDRE assessed as growth hormone level by transcriptional assay, ED50 = 0.0015 μM.	17924616
HEK293	Function assay		24 hrs	Transactivation of recombinant human VDR/RXRalpha expressed in HEK293 cells after 24 hrs by Dual-luciferase reporter gene assay, EC50 = 0.00158 μM.	30193216
MCF7	Function assay		24 hrs	Agonist activity at VDR in human MCF7 cells assessed as increase in transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay, EC50 = 0.0016 μM.	29733645
MCF10DCIS.com	Antiproliferative assay		3 days	Antiproliferative activity against ER positive human MCF10DCIS.com cells after 3 days by [3H]thymidine uptake assay, IC50 = 0.00175 μM.	22180837
HL60	Function assay			Induction of differention of human HL60 cells into monocytes by NBT reduction assay, EC50 = 0.002 μM.	17960924
HL-60	Function assay		4 days	Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay, EC50 = 0.002 μM.	18722130
bone marrow cells	Function assay		3 days	Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days, EC50 = 0.002 μM.	18539034
HL60	Function assay		4 days	Induction of differentiation of human HL60 cells promyelocytes to monocytes after 4 days by NBT reduction assay, Ki = 0.002 μM.	21105677
HeLa	Function assay		18 hrs	Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM.	22957834
PBMC	Function assay			In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation, ED50 = 0.0027 μM.	11000014
HL60	Function assay			Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay, EC50 = 0.003 μM.	19167893
HEK293	Function assay			Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay, EC50 = 0.003 μM.	23462715
MCF7	Function assay		24 hrs	Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay, EC50 = 0.00328 μM.	22989379
Caco-2	Function assay			Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum, EC50 = 0.00352 μM.	18054230
MCF10AT1	Antiproliferative assay		3 days	Antiproliferative activity against ER positive human MCF10AT1 cells after 3 days by [3H]thymidine uptake assay, IC50 = 0.0039 μM.	22180837
Jurkat	Function assay		24 hrs	Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay, EC50 = 0.003936 μM.	27070779
MCF7	Function assay			Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay, EC50 = 0.0055 μM.	22180837
MCF10CA1a	Antiproliferative assay		3 days	Antiproliferative activity against ER positive human MCF10CA1a cells after 3 days by [3H]thymidine uptake assay, IC50 = 0.0062 μM.	22180837
HL60	Function assay		96 hrs	Agonist activity at VDR in human HL60 cells assessed as induction of cell differentiation after 96 hrs by NBT assay, EC50 = 0.009 μM.	29518319
HL-60	Function assay		96 hrs	Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis, EC50 = 0.009 μM.	26562542
THP1	Function assay			Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR, EC50 = 0.01 μM.	19309155
THP1	Function assay			Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR, EC50 = 0.01 μM.	19309155
ROS 17/2.8	Function assay			Effective dose for transcriptional activation in ROS 17/2.8 osteosarcoma cells, ED50 = 0.01 μM.	10893309
HL60	Function assay		144 hrs	Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay, IC50 = 0.05 μM.	25180926
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay, EC50 = 0.052 μM.	19739672
bone marrow cells	Function assay		3 days	Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3, EC50 = 0.1 μM.	18539034
HL-60	Function assay			Inhibition of colony formation assays on HL-60 cells, ED50 = 0.13 μM.	10893309
Caco2	Function assay		24 hrs	Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay, EC50 = 0.2234 μM.	27070779
HaCaT	Function assay		24 hrs	Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay, EC50 = 0.2497 μM.	27070779
HaCaT	Function assay		24 hrs	Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.3215 μM.	26367019
MCF-7	Function assay			Inhibition of colony formation assays on MCF-7 cells, ED50 = 0.38 μM.	10893309
CV1	Function assay			Effect on VDR-mediated transcriptional activity in CV1 cells transfected with human recombinant VDR, ED50 = 0.4 μM.	15615534
Caco2	Function assay		24 hrs	Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.5152 μM.	26367019
HN12	Antiproliferative assay		72 hrs	Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.553 μM.	24900339
L02	Antiproliferative assay		48 hrs	Antiproliferative activity against human L02 cells after 48 hrs by MTT assay, IC50 = 0.67 μM.	29518319
L02	Cytotoxicity assay		48 hrs	Cytotoxicity against human L02 cells after 48 hrs by MTT assay, IC50 = 0.67 μM.	26562542
Caco2	Antiproliferative assay		48 hrs	Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay, IC50 = 4.4 μM.	26562542
Caco2	Antiproliferative assay		48 hrs	Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay, IC50 = 4.46 μM.	29518319
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 5.59 μM.	29518319
MCF7	Antiproliferative assay		48 hrs	Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 5.6 μM.	26562542
MCF7	Function assay		16 hrs	Binding affinity to VDR in scrambled siRNA-transfected human MCF7 cells assessed as cell growth inhibition by measuring reduction in BrdU incorporation after 16 hrs by ELISA, IC50 = 6.43 μM.	30193216
PC3	Antiproliferative assay		24 hrs	Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay, IC50 = 9.53 μM.	30193216
MCF7	Antiproliferative assay		24 hrs	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 11.43 μM.	30193216
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay, IC50 = 12.5 μM.	25127149
PC3	Antiproliferative assay		48 hrs	Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 17.2 μM.	26562542
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 17.25 μM.	29518319
BxPC3	Antiproliferative assay		24 hrs	Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay, IC50 = 21.07 μM.	30193216
PBMC	Function assay	10 nM	up to 8 hrs	Activation of VDR in LPS-stimulated human PBMC cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression at 10 nM after upto 8 hrs by RT-PCR	19309155
THP1	Function assay			Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression at EC50 upto 5 hrs by RT-PCR	19309155
NB4	Function assay	1 nM	48 hrs	Induction of cell differentiation in human NB4 cells assessed as induction of induction of cell surface marker CD14 expression at 1 nM after 48 hrs	19685888
NB4	Function assay	1 nM	48 hrs	Induction of cell differentiation in human NB4 cells assessed as induction of induction of cell surface marker CD11b expression at 1 nM after 48 hrs	19685888
HL60	Function assay		4 days	Induction of cell differentiation in human HL60 cells after 4 days by NBT reduction assay	19193059
HL60	Function assay	10 μM		Inhibition of 1,25-(OH)2D3-induced cell differentiation in human HL60 cells assessed as morphological changes at 10'-6 M by Wright-Geimsa staining	19193059
SCC4	Function assay	1 uM	5 to 10 mins	Agonist activity at VDR in human SCC4 cells assessed as induction of CYP24 gene expression at 1 uM after 5 to 10 mins by RT-PCR analysis	20452225
SCC25	Function assay	10 nM		Agonist activity at VDR in human SCC25 cells assessed as induction of CYP24 expression at 10 nM	20883026
SCC25	Function assay	100 nM		Agonist activity at VDR in human SCC25 cells assessed as induction of TSLP expression at 100 nM	20883026
C3H10T1/2	Function assay	0.5 to 5 uM	24 hrs	Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as down regulation of Gli1 at 0.5 to 5 uM after 24 hrs by RT-PCR analysis	22226657
HL60	Function assay	1 μM		Induction of vitamin D receptor-mediated differentiation of human HL60 cells at 10'-5 M by NBT reduction method	22285943
HL60	Function assay	1 nM to 10 μM		Induction of vitamin D receptor-mediated differentiation of human HL60 cells at 10'-9 to 10'-5 M by NBT reduction method	22285943
A498	Function assay	10 nM	4 hrs	Induction of CYP24 mRNA expression in human A498 cells at 10'-8 M after 4 hrs by RT-PCR analysis	21392983
A498	Function assay	10 nM	16 hrs	Induction of CYP24 mRNA expression in human A498 cells at 10'-8 M after 16 hrs by RT-PCR analysis	21392983
DU145	Function assay	7.5 uM	18 hrs	Agonist activity at VDR-LBD in human DU145 cells assessed as CYP24A1 expression at 7.5 uM after 18 hrs by qRT-PCR method	26774929
HaCaT	Function assay			Inhibition of colony formation of human HaCaT cells	22404326
HCT116	Function assay	20 to 40 uM	24 hrs	Agonist activity at RAR (unknown origin) expressed in human HCT116 cells co-expressing RARE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay	23276449
HCT116	Function assay	20 to 40 uM	24 hrs	Agonist activity at RXR (unknown origin) expressed in human HCT116 cells co-expressing RXRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay	23276449
HEK293	Function assay	100 nM	24 hrs	Induction of cyp24A1 mRNA expression in HEK293 cells at 100 nM after 24 hrs by real-time PCR	24773565
HEK293	Function assay	10 nM		Transactivation of human VDR D149A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay	24818857
HEK293	Function assay	10 nM		Transactivation of human VDR K240A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay	24818857
MCF7	Antitumor assay	0.5 mg/kg	3 weeks	Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in p21 expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an	30193216
MCF7	Antitumor assay	0.5 mg/kg	3 weeks	Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in p27 expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an	30193216
MCF7	Antitumor assay	0.5 mg/kg	3 weeks	Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation	30193216
MCF7	Antitumor assay	0.5 mg/kg	3 weeks	Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in Bax expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an	30193216
C3H10T1/2	Function assay	0.5 uM	24 hrs	Activation of hedgehog signaling pathway in non-targeting siRNA treated mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis	24730984
C3H10T1/2	Function assay	0.5 uM	24 hrs	Activation of hedgehog signaling pathway in VDR-knockdown mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis	24730984
C3H10T1/2	Function assay	0.5 uM	24 hrs	Effect on CYP24A1 RNA level in non-targeting siRNA treated mouse C3H10T1/2 cells at 0.5 uM after 24 hrs by qPCR analysis	24730984
C3H10T1/2	Function assay	0.5 uM	24 hrs	Inhibition of hedgehog signaling pathway in non-targeting siRNA treated mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis	24730984
C3H10T1/2	Function assay	0.5 uM	24 hrs	Inhibition of hedgehog signaling pathway in VDR-knockdown mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis	24730984
LX2	Function assay	100 nM	24 hrs	Transactivation of VDR in human LX2 cells assessed as inhibition of TGFbeta1-induced COL1A1 mRNA expression at 100 nM after 24 hrs by Q-PCR analysis	30350999
ROS 17/2.8	Function assay		16 hrs	Induction of VDR transcriptional activity assessed as activation of 24-hydroxylase gene expression in rat ROS 17/2.8 cells after 16 hrs by luciferase reprter assay	26574921
HL60	Function assay	30 to 1000 nM	48 hrs	Induction of cell differentiation in human HL60 cells assessed as maturing morphological changes at 30 to 1000 nM after 48 hrs by Wright's-Giemsa staining-based forty microscopic view assay	25127149
SW480-ADH	Function assay	100 nM	48 hrs	Induction of human SW480-ADH cell differentiation assessed as formation of compact epithelioid islands of highly adherent cells at 10 '-7 M after 48 hrs by phase-contrast microscopy	22989379
SW480-ADH	Function assay	10 nM	48 hrs	Induction of human SW480-ADH cell differentiation assessed as formation of compact epithelioid islands of highly adherent cells at 10 '-8 M after 48 hrs by phase-contrast microscopy	22989379
MCF7	Antiproliferative assay	100 nM	48 hrs	Antiproliferative activity against human MCF7 cells at 10 '-7 M after 48 hrs by MTT assay relative to untreated-control	22989379
CLL	Function assay	100 nM	24 hrs	Effect on CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated GADD45alpha mRNA expression at 100 nM incubated for 24 hrs by quantitative RT-PCR method	25148392
CLL	Function assay	100 nM	24 hrs	Effect on CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated CDKN1A mRNA expression at 100 nM incubated for 24 hrs by quantitative RT-PCR method	25148392
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Biological Activity

Description

Targets

vitamin D receptor ^[1]
(Cell-free assay)

In vitro
In vitro	Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion. ^[1] Calcitriol increases the concentration of intracellular calcium ([Ca2+]i) within 5 s by mobilizing calcium from the endoplasmic reticulum and the formation of inositol 1,4, 5-trisphosphate and diacylglycerol. ^[2] Calcitriol can inhibit the proliferation and promote the differentiation of human prostate adenocarcinoma cells. Calcitriol causes a selective decrease in the secreted levels of type IV collagenases (MMP-2 and MMP-9). ^[3] Calcitriol has antiproliferative activity in squamous cell carcinoma and prostatic adenocarcinoma and enhances the antitumor activity of platinum-based agents. Calcitriol prior to paclitaxel significantly reduces clonogenic survival compared with either agent alone in the murine squamous cell carcinoma and PC-3 cells. ^[4] Calcitriol is a potent anti-proliferative agent in a wide variety of malignant cell types. Calcitriol effects are associated with an increase in G0/G1 arrest, induction of apoptosis and differentiation, modulation of expression of growth factor receptors. Calcitriol potentiates the antitumor effects of many cytotoxic agents and inhibits motility and invasiveness of tumor cells and formation of new blood vessels. ^[5]
Cell Research	Cell lines	CLL cells
	Concentrations	100 nM
	Incubation Time	24 h
	Method	CLL cells were treated with DMSO (vehicle control) or calcitriol (100 nM). Cells were harvested at the indicated time points with mild trypsinization
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	CyclinD1 IRE1α / p-eIF2α / eIF2α / Atf4 / CHOP p-PERK / PERK FGFR1 / FGFR2 / FGFR3 / FGFR4 Wnt10b / Wnt16		28643892

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06169397	Not yet recruiting	Pulmonary Sarcoidosis	Xentria Inc.	January 2024	Phase 2
NCT04551170	Recruiting	Pseudohypoparathyroidism\|Albright Hereditary Osteodystrophy\|Pseudohypoparathyroidism Type 1a	Vanderbilt University Medical Center	July 13 2020	Phase 2
NCT03029429	Recruiting	Pseudohypoparathyroidism\|Albright Hereditary Osteodystrophy	Vanderbilt University Medical Center\|Harvard University	September 1 2018	Phase 2

References

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Chemical lnformation & Solubility

Molecular Weight	416.64	Formula	C₂₇H₄₄O₃
CAS No.	32222-06-3	SDF	Download Calcitriol SDF
Smiles	CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C
Storage (From the date of receipt)	1 year -80°C powder（in dark and seal）	Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt.

In vitro
Batch:

DMSO : 83 mg/mL ( (199.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):