罗格列酮

一般描述

Rosiglitazone is a member of the thiazolidinedione family. It effectively lowers glucose levels by enhancing the response of target cells to insulin, without causing increased stimulation and release of insulin by the pancreatic beta cells. Rosiglitazone functions by activating the nuclear peroxisome proliferator-activated (PPAR) receptor gamma, which plays a key role in regulating adipogenesis, glucose metabolism, and genetic networks. It exhibits high potency as a thiazolidinedione, with a binding affinity for PPAR-gamma that is 30-fold higher than pioglitazone. Furthermore, it increases insulin-stimulated IRS-1/2 in skeletal muscle and adipose tissue, leading to the expression of the GLUT4 glucose transporter.

应用

罗格列酮已被用于：

· 脂肪细胞分化的培养基成分

· 人结肠癌细胞的细胞增殖测定

· 脂肪细胞中Bcl-2样蛋白13（Bcl2113）的表达

· 作为过氧化物酶体增殖物激活受体γ（PPARγ）的配体

生化/生理作用

罗格列酮是PPARγ的强效激动剂，对人受体的EC50为43 nM。 它是一种抗糖尿病药，作为胰岛素增敏剂，可与脂肪细胞的PPARγ受体结合并使细胞对胰岛素更敏感。