Dapagliflozin

Research use only, not for human use.

A potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM.

A potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM; displays >300-fold selectivity over hSGLT1 (EC50=330 nM), highly selectivity versus GLUT transporters; also is a potent selective inhibitor of rSGLT2 (EC50=3 nM), with 200-fold selectivity versus rSGLT1; significantly improves glucose homeostasis, reduces blood glucose levels in hyperglycemic streptozotocin (STZ) rats.Diabetes Approved(In Vitro):Dapagliflozin (0-10 μM；24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.Dapagliflozin (0-10 μM；2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells..(In Vivo):Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis.

Dapagliflozin (0-10 μM；24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.Dapagliflozin (0-10 μM；2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells.Cell Viability Assay Cell Line:Hypoxic HK2 cells Concentration:0 μM, 1 μM, 2 μM, 5 μM, 10 μM Incubation Time:24 hours Result:Improved the cell viability in a dose-dependent manner compared with control cells.Western Blot Analysis Cell Line:Hypoxic HK2 cells, Normoxic HK2 cells Concentration:0 μM, 1 μM, 2 μM, 5 μM, 10 μM Incubation Time:24 hours Result:Induced HIF1 expression in hypoxic and normoxic HK2 cells.

Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis.

BMS-512148 | BMS512148 | BMS 512148

GPCR/G Protein

SGLT

hSGLT2

Metabolic Disease

Diabetes

461432-26-8

408.8726

C21H25ClO6

>98% (HPLC)

10 mM in DMSO

O[C@H]1[C@H](C2=CC=C(Cl)C(CC3=CC=C(OCC)C=C3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O

D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-, (1S)-

(-20℃)

With Ice Pack

≥ 2 years