Dapagliflozin (BMS-512148), a new type of drug used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine.
Dapagliflozin induces HIF1 expression and attenuates renal IR injury.
IC50&Target
SGLT2
体外研究
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.
体内研究
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.
分子式
C21H25ClO6
分子量
408.87
CAS号
461432-26-8
中文名称
达格列净;达帕格列净;达格列嗪
运输条件
Room temperature in continental US; may vary elsewhere.