Troglitazone

Troglitazone is a selective agonist of peroxisome proliferator-activated receptor ? (PPAR?; EC50s = 0.78 and 0.55 ?M for the mouse and human receptors, respectively, in a transactivation assay).{10670} It is selective for PPAR? over PPAR? and PPAR?, at which it is inactive at concentrations up to 10 ?M. Troglitazone (500 mg/kg twice per day) exhibits antihyperglycemic and antihyperlipidemic properties in Zucker diabetic fatty rats, reducing plasma glucose and triglyceride levels by 61 and 87% respectively.{25251} It also induces cell cycle arrest at the G1 phase in SK-HEP-1 and Hep3B hepatocellular carcinoma cells when used at a concentration of 10 ?M and increases apoptosis in these cells at concentrations of 30 ?M and higher.{10669}