产品描述:
MSDC-0602 is a PPARγ-sparing thiazolidinedione derivative.{43414} It binds only weakly to PPARγ (IC50 = 18.25 µM) and induces minimal activation of a Gal4-PPARγ reporter construct when used at a concentration of 50 µM. MSDC-0602 binds to mitochondrial membranes and decreases the pyruvate-induced oxygen consumption rate in control mitochondria but not in liver-specific mitochondrial pyruvate carrier 2 knockout (LS-Mpc2-/-) mitochondria.{43423} It reduces body weight gain and adiposity, as well as increases intrascapular brown adipose tissue (BAT) mass in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a high-trans-fat, -fructose, and -cholesterol diet when administered in the diet for 12 weeks, starting four weeks after the beginning of the diet.{43424} It also reverses hepatic fibrosis and stellate cell fibrinogenesis when administered for three weeks, starting 16 weeks after the beginning of the diet. MSDC-0602 decreases plasma glucose, triglyceride, and cholesterol levels in ob/ob mice and increases insulin sensitivity in the striatal muscle, adipose tissue, and liver of diet-induced obese mice.{43414}