| 名称 | GSK1292263 |
| 描述 | GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2. |
| 激酶实验 | 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. |
| 体外活性 | In male Sprague-Dawley rats, GSK-1292263 (3-30 mg/kg) was associated with increased levels of gastrointestinal peptides, including glucagon-like peptide 1, oxyntomodulin, peptide YY, and glucagon, especially in the absence of nutrients. This increase was further enhanced by oral glucose administration during glucose tolerance tests. In a 6-week study on Zucker diabetic fatty rats, GSK-1292263 led to a statistically significant increase in insulin immunoreactivity in pancreatic sections compared to the blank control. Furthermore, in a hyperinsulinemic-normoglycemic clamp experiment in Sprague-Dawley rats, GSK-1292263 (10/30 mg/kg) stimulated glucagon secretion without raising blood glucose levels when administered 2 hours before insulin injection, in comparison to the vehicle control. |
| 体内活性 | Utilizing Hypo1, GSK-1292263 was identified from a pool of 1,538 compounds. The Fit-Value of GSK-1292263 corresponding to Hypo1 and its estimated value were 8.8 and 7.7 nM, respectively. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 32 mg/mL (70.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
|
| 关键字 | diabetes | type | mellitus | GSK 1292263 | GPR119 | inhibit | G Protein-Coupled Receptor 119 | T2DM | Inhibitor | GSK-1292263 | GSK1292263 |
| 相关产品 | Vincamine | Monomethyl fumarate | Questiomycin A | 3-Hydroxyoctanoic Acid | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | Timapiprant | NF-56-EJ40 |
| 相关库 | 表型筛选靶点鉴定库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 抗肥胖化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 内分泌激素分子库 | 已知活性化合物库 | GPCR靶点分子库 | 抗癌药物库 |
United States
