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]

羅格列酮已被用于：

• 脂肪細(xì)胞分化的培養(yǎng)基成分[2]
• 人結(jié)腸癌細(xì)胞的細(xì)胞增殖測定[3]
• 脂肪細(xì)胞中Bcl-2樣蛋白13（Bcl2113）的表達(dá)[4]
• 作為過氧化物酶體增殖物激活受體γ（PPARγ）的配體[5]

羅格列酮是PPARγ的強(qiáng)效激動(dòng)劑，對(duì)人受體的EC50為43 nM。 它是一種抗糖尿病藥，作為胰島素增敏劑，可與脂肪細(xì)胞的PPARγ受體結(jié)合并使細(xì)胞對(duì)胰島素更敏感。

《受體分類和信號(hào)轉(zhuǎn)導(dǎo)》手冊的 AMPK 和 核受體（PPAR） 頁面有該化合物的介紹。想要瀏覽手冊的其他頁面， 請(qǐng)單擊此處。

該化合物是ADME Tox和基因調(diào)控研究的特色產(chǎn)品。發(fā)現(xiàn)更多 ADME Tox 和 基因調(diào)控 特色產(chǎn)品。想要了解有關(guān)生物活性小分子在其他研究域應(yīng)用的更多信息，請(qǐng)?jiān)L問 sigma.com/discover-bsm。

該化合物由 GlaxoSmithKline開發(fā)。想要瀏覽其他由制藥公司開發(fā)的化合物以及已批準(zhǔn)物/候選藥物清單， 請(qǐng)單擊此處。