标题罗格列酮

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.[1]

罗格列酮已被用于：

• 脂肪细胞分化的培养基成分[2]
• 人结肠癌细胞的细胞增殖测定[3]
• 脂肪细胞中Bcl-2样蛋白13（Bcl2113）的表达[4]
• 作为过氧化物酶体增殖物激活受体γ（PPARγ）的配体[5]

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。

《受体分类和信号转导》手册的 AMPK 和 核受体（PPAR） 页面有该化合物的介绍。想要浏览手册的其他页面， 请单击此处。

该化合物是ADME Tox和基因调控研究的特色产品。发现更多 ADME Tox 和 基因调控 特色产品。想要了解有关生物活性小分子在其他研究域应用的更多信息，请访问 sigma.com/discover-bsm。

该化合物由 GlaxoSmithKline开发。想要浏览其他由制药公司开发的化合物以及已批准物/候选药物清单， 请单击此处。