GSK1292263 是口服具有活性的 GPR119 激动剂，对人和大鼠 GPR119的pEC50分别为 6.9 和 6.7，它可用于研究 2 型糖尿病 (T2DM) 。

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

在雄性Sprague-Dawley大鼠体内,营养素不存在时,GSK-1292263（3-30 mg/kg）与循环胃肠肽、包括胰高血糖素样多肽1、肠抑胃肽、多肽YY和胰高血糖素水平的增加相关,在口服葡萄糖耐量测试中,葡萄糖给药对循环胃肠肽的增加有加强作用.在Zucker糖尿病肥胖大鼠的6周研究中,与空白对照相比,GSK-1292263与胰腺切片中胰岛素免疫反应性出现具有统计学意义的显著增加有关.在Sprague-Dawley大鼠体内,高胰岛素-正常血糖钳夹实验中,胰岛素注射2 h前,与载体对照相比,GSK-1292263（10/30 mg/kg）刺激胰高血糖素分泌,但不增加血糖水平.

使用Hypo1从1538个化合物中发现GSK-1292263,GSK-1292263与Hypo1匹配的Fit-Value和估计值分别为8.8和7.7 nM。

FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.

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C23H28N4O4S

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Ethanol:<1 mgml
DMSO:32 mg/mL (70.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years