Dapagliflozin is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

在高血糖链脲佐菌素大鼠中,口服 Dapagliflozin（0.1 mg/kg）能够降低血糖水平.在Zucker糖尿病肥胖大鼠中,Dapagliflozin对于肝脏和肾脏表现出良好的安全性,能够降低葡萄糖水平.

在体外代谢通路中,Dapagliflozin能够参与糖脂化,羟乙基化,脱乙基作用。在大鼠,犬,猴,人类血清中,Dapagliflozin（10 μM ）能够稳定发挥作用。在无蛋白buffer中,Dapagliflozin（20 μM）能够选择性地作用于GLUT转运蛋白

To perform the cell survival assay, cells are collected after 24 h incubation with vehicle or dapagliflozin pretreatment in 30-min ischemia and surviving cells are counted with Trypan blue staining. The percentage survival is determined by quantization of the relative viable number of treated cells divided by the viable number of untreated cells.

461432-26-8

C21H25ClO6

408.87

BMS-512148;达格列净;Dapagliflozin

[1]Meng W, et al. J Med Chem, 2008, 51(5), 1145-1149. [2]Obermeier M, et al. Drug Metab Dispos, 2010, 38(3), 405-414. [3]Chiba Y, et al. Dapagliflozin, a Sodium-Glucose Co-Transporter 2 Inhibitor, Acutely Reduces Energy Expenditure in BAT via Neural Signals in Mice. PLoS One. 2016 Mar 10;11(3):e0150756. [4]Macdonald FR, et al. Diabetes Obes Metab, 2010, 12(11), 12004-12012. [5]Chang YK, et al. Dapagliflozin, SGLT2 Inhibitor, Attenuates Renal Ischemia-Reperfusion Injury. PLoS One. 2016 Jul 8;11(7):e0158810. [6]Han S, et al. Diabetes, 2008, 57(6), 1723-1729.

[1]Xuan M Y, Piao S G, Ding J, et al. Dapagliflozin Alleviates Renal Fibrosis by Inhibiting RIP1-RIP3-MLKL-Mediated Necroinflammation in Unilateral Ureteral Obstruction. Frontiers in pharmacology. 2021, 12

Ethanol:14 mg/mL (34.2 mM)
H2O:<1 mg/mL
DMSO:76 mg/mL (185.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years