Tofogliflozin hydrate 是一种有效的，选择性的SGLT2抑制剂，IC50为 2.9 nM，对人、大鼠和小鼠SGLT2的Ki分别为 2.9 nM，14.9 nM 和 6.4 nM。Tofogliflozin hydrate 对肾小管细胞中高葡萄糖诱导的ROS生成具有部分抑制作用。

Tofogliflozin hydrate is a potent and highly specific inhibitor of SGLT2(IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2).

Tofogliflozin, a highly selective inhibitor of SGLT2 on oxidative stress generation, inflammatory and proapoptotic reactions in cultured human proximal tubular cells exposed to high glucose.?Tofogliflozin dose-dependently suppressed glucose entry into tubular cells.?High glucose exposure (30 mM) for 4 and 24 h significantly increased oxidative stress generation in tubular cells, which were suppressed by the treatment of tofogliflozin or an antioxidant N-acetylcysteine (NAC).?Monocyte chemoattractant protein-1 (MCP-1) gene expression and apoptotic cell death were induced by 4 h- and 8 day-exposure to high glucose, respectively, both of which were also blocked by tofogliflozin or NAC.?The present study suggests that SGLT2-mediated glucose entry into tubular cells could stimulate oxidative stress and evoke inflammatory and proapoptotic reactions in this cell type.?Blockade of glucose reabsorption in tubular cells by SGLT2 inhibitor might exert beneficial effects on tubulointerstitial damage in diabetic nephropathy[1].

1201913-82-7

C22H28O7

404.459

Tofogliflozin hydrate;CSG-452 hydrate;托格列净

DMSO:90 mg/mL (222.52 mM)
H2O:0.33 mg/mL (0.82 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years