Home GPCR & G Protein SGLT inhibitor Dapagliflozin For research use only.

Dapagliflozin

Synonyms: BMS-512148

Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.

Dapagliflozin Chemical Structure

Dapagliflozin Chemical Structure

CAS: 461432-26-8

Selleck's Dapagliflozin has been cited by 36 publications

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
CHO cells Function assay 2 h Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50=0.00049 μM 20434909
CHOK1 cells Function assay 3 h Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis, IC50=0.001 μM 24842618
HEK293.ETN cells Function assay 1.5 h Inhibition of human SGLT2 transfected in HEK293.ETN cells assessed as AMG uptake after 1.5 hrs by scintillation counting, IC50=0.0067 μM 19896374
COS-7 cells Function assay 2 h Inhibition of human SGLT1 transfected in COS-7 cells assessed as AMG uptake after 2 hrs by scintillation counting, IC50=0.89 μM 19896374
CHO Function assay Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 0.0011 μM. 18260618
CHO Function assay Inhibition of rat SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 0.003 μM. 18260618
CHO Function assay Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 1.39 μM. 18260618
HEK293.ETN Function assay Inhibition of human SGLT2 expressed in HEK293.ETN cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting, IC50 = 0.0067 μM. 19700318
COS7 Function assay Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting, IC50 = 0.885 μM. 19700318
HEK293 Function assay Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake, IC50 = 0.81 μM. 19785435
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs, IC50 = 0.0014 μM. 20149653
CHO Function assay 2 hrs Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs, IC50 = 1.2 μM. 20149653
CHO Function assay Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting, IC50 = 0.00049 μM. 20181486
HEK293 Function assay 1.5 hrs Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting, IC50 = 0.0067 μM. 20576578
COS7 Function assay 2 hrs Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.89 μM. 20576578
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, EC50 = 0.003 μM. 21128592
CHO Function assay 2 hrs Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, EC50 = 0.4285 μM. 21128592
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. 21193308
CHO Function assay 60 mins Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.004 μM. 21398124
CHO Function assay 60 mins Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma, IC50 = 0.022 μM. 21398124
CHO Function assay 60 mins Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.37 μM. 21398124
CHO Function assay 60 mins Inhibition of SGLT6 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.38 μM. 21398124
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counter, IC50 = 0.00049 μM. 21514014
CHO Function assay 60 mins Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting, IC50 = 0.003 μM. 21565497
CHO Function assay Inhibition of human SGLT2 expressed in CHO cells using methyl-alpha-D-glucopyranoside by liquid scintillation counting, IC50 = 0.00135 μM. 21592794
COS7 Function assay 2 hrs Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma, IC50 = 0.0032 μM. 21737266
293 Function assay 1.5 hrs Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma, IC50 = 3.1 μM. 21737266
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as reduction of [14C]-labeled AMG after 2 hrs by liquid scintillation counting, IC50 = 0.00135 μM. 21868239
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. 21906953
CHO-K1 Function assay Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50 = 0.0013 μM. 22652255
CHO-K1 Function assay Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50 = 0.8 μM. 22652255
CHO-K1 Function assay 120 mins Inhibition of human SGLT2 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay, EC50 = 0.0024 μM. 22818040
CHO-K1 Function assay 120 mins Inhibition of human SGLT1 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay, EC50 = 0.593 μM. 22818040
CHO Function assay 45 mins Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins, IC50 = 0.0013 μM. 22889351
CHO Function assay 45 mins Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins, IC50 = 0.8 μM. 22889351
CHOK1 Function assay 3 hrs Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis, IC50 = 0.891 μM. 24842618
CHO Function assay 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. 24900297
CHO Function assay 2 hrs Competitive inhibition of full-length human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by scintillation counting, IC50 = 0.005 μM. 25650254
CHO Function assay 120 mins Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method, IC50 = 0.0015 μM. 28447791
CHO Function assay 120 mins Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method, IC50 = 0.629 μM. 28447791
CHO Function assay 1 hr Inhibition of human SGLT2 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method, EC50 = 0.002 μM. 29216560
CHO Function assay 1 hr Inhibition of human SGLT1 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method, EC50 = 0.86 μM. 29216560
CHO Function assay 1 hr Inhibition of full-length human SGLT2 expressed in CHO cells assessed as decrease in [14C]-methyl alpha-D-glucopyranoside uptake after 1 hr by liquid scintillation counting method, IC50 = 0.00105 μM. 29764742
HEK293 Function assay 10 mins Inhibition of human SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method, IC50 = 0.0014 μM. 29954682
HEK293 Function assay 10 mins Inhibition of human SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method, IC50 = 1.83 μM. 29954682
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Biological Activity

Description Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Features More potent stimulator of glucosuria than other SGLT2 inhibitors.
Targets
hSGLT2 [1]
(CHO cells)
1.1 nM(EC50)
In vitro
In vitro

Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. [1]

Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly selective versus GLUT transporters and displays 8–9% inhibition in protein-free buffer at 20 μM and virtually no inhibition in the presence of 4% bovine serum albumin. [2]

Dapagliflozin has good permeability across Caco-2 cell membranes and is a substrate for P-glycoprotein (P-gp) but not a significant P-gp inhibitor. Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM. Dapagliflozin shows no inhibitory responses or induction to human P450 enzymes. The in vitro metabolic pathways Dapagliflozin are glucuronidation, hydroxylation, and O-deethylation. [3]
Kinase Assay SGLT Binding Assays
Chinese hamster ovary (CHO) cells stably expressing human SGLT2 (hSGLT2) and human SGLT1 (\hSGLT1) are utilized for the development of transport assays using the selective SGLT substrate α-methyl-D-glucopyranoside (AMG). Dapagliflozin is assayed for the ability to inhibit [14C]AMG uptake in a protein- free buffer over a 2 hours incubation period. The response curve is fitted to an empirical four-parameter model to determine the inhibitor concentration at half maximal response, reported as EC50. Protein-free buffer is used to simulate the low-protein conditions of the glomerular filtrate, which bathes the SGLT targets on the lumenal surface of the proximal tubule in the kidney.
Experimental Result Images Methods Biomarkers Images PMID
Western blot HIF-1α / p-AMPK / AMPK / p-ERK / ERK / β-actin DDR1 HIF-1α / PHD2 / tubulin p-elf2α / t-elf2α / tubulin-α Bax / Bcl2 / PARP / β-actin 27391020
Growth inhibition assay Tumor volume 28763435
IHC TUNEL-positive cells HIF1 TUNEL-positive cells mice kidney sections HE staining / SGLT2 27391020
Immunofluorescence Metabolic switch in diabetic kidneys F-actin EdU PECAM-1 / α-SMA podocytes 32444604
In Vivo
In vivo

Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the metabolic stability conferred by the C-glucoside linkage. Dapagliflozin displays a favorable absorption, distribution, metabolism, and excretion (ADME) profile and is orally bioavailable. [1]

Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and increase in urine volume in normal rats over 24 hours post-dose. Dapagliflozin induces increase in urine glucose and urine volume excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats. Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2 weeks of treatment, without any marker of renal or liver toxicity. [2]

Dapagliflozin significantly reduces the development of hyperglycaemia, with lowered blood glucose. Dapagliflozin could improve the insulin sensitivity, reduce β-cell mass and the development of impaired pancreatic function. [4]
Animal Research Animal Models Normal Sprague Dawley rats or streptozotocin induced male Sprague Dawley rats
Dosages 0.01-10 mg/kg (1 mL/kg) followed by a 50% glucose solution (2 g/kg)
Administration Dosed orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06012266 Not yet recruiting Heart Failure Centre Hospitalier Universitaire Vaudois|Great Ormond Street Hospital for Children NHS Foundation Trust|University College London January 2024 Phase 2
NCT06000462 Not yet recruiting Obesity|Dapagliflozin Adverse Reaction|Weight Loss|Effect of Drug Oman Ministry of Health December 2023 Phase 2|Phase 3
NCT04887935 Not yet recruiting Prostate Cancer|Cancer of Prostate Washington University School of Medicine December 31 2023 Phase 1
NCT06165601 Not yet recruiting Chronic Kidney Diseases University Hospital Montpellier December 1 2023 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 408.87 Formula

C21H25ClO6
CAS No. 461432-26-8 SDF Download Dapagliflozin SDF
Smiles CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl
Storage (From the date of receipt) 3 years -20°C powder (seal)

In vitro
Batch:

DMSO : 100 mg/mL ( (244.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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