Troglitazone

PPARγ的选择性激动剂（在转录激活试验中，小鼠和人类受体的EC50s分别为0.78和0.55μM）；对PPARγ的选择性优于PPARα和PPARδ，当≤10μM时，该药物无活性；在Zucker糖尿病肥胖大鼠中表现出抗高血糖和抗高血脂特性，每天两次500mg/kg剂量下，血浆葡萄糖和甘油三酯水平分别降低61%和87%；在10μM时，诱导SK-HEP-1和Hep3B肝细胞癌细胞的细胞周期停滞于G1期，在≥30μM时，增加这些细胞的凋亡。A selective agonist of PPARγ (EC50s = 0.78 and 0.55 μM for the mouse and human receptors, respectively, in a transactivation assay); selective for PPARγ over PPARα and PPARδ, at which it is inactive at ≤10 μM; exhibits antihyperglycemic and antihyperlipidemic properties in Zucker diabetic fatty rats, reducing plasma glucose and triglyceride levels by 61 and 87% respectively, at 500 mg/kg twice per day; induces cell cycle arrest at the G1 phase in SK-HEP-1 and Hep3B hepatocellular carcinoma cells at 10 μM and increases apoptosis in these cells at ≥30 μM.分子式C24H27NO5S分子量441.5O=C1NC(=O)C(S1)Cc1ccc(cc1)OCC1(C)CCc2c(O1)c(C)c(C)c(O)c2C