GSK1292263

• 产品号: S2149
• CAS号: 1032823-75-8
• 分子式: C23H28N4O4S
• 分子量: 456.55782
• 保 存: -20°C

产品别名

• 标题: GSK1292263
• IUPAC标准名: 2-(4-methanesulfonylphenyl)-5-({1-[3-(propan-2-yl)-1,2,4-oxadiazol-5-yl]piperidin-4-yl}methoxy)pyridine
• IUPAC传统名: 5-{[1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl]methoxy}-2-(4-methanesulfonylphenyl)pyridine

产品登记号

• CAS号: 1032823-75-8

产品性质

• 作用靶点: GPR
• 成盐信息: Free Base
• 保存条件: -20°C

产品详细信息

详细说明 (English)

Research Area

• Description: Hyperlipidaemia ,Type-2 diabetes mellitus

Biological Activity

• Description: GSK-1292263 is a novel GPR119 agonist.
• Targets: GPR119
• In Vitro: GSK-1292263 is selected from 1538 compounds by using Hypo1, the Fit-Value and Estimate of GSK-1292263 that is aligned in Hypo1 are 8.8 and 7.7 (nM), respectively. ^[1]
• In Vivo: GSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including glucagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and glucagon in male Sprague-Dawley rats, the increase is enhanced following administration of glucose in the oral glucose tolerance test (OGTT). GSK-129226 significant increases in the peak insulin response and insulin AUC(0-15 min) of 30-60% compared with values in the vehicle control cohort in the intravenous glucose tolerance test in rats, this insulin upregulation correlated with a significant increase in the glucose disposal rate. GSK-1292263 is associated with a statistically significant increase in insulin immunoreactivity in pancreatic sections in a 6-week study performed in Zucker diabetic fatty rats, compared with insulin immunoreactivity in samples obtained from rats receiving vehicle control. GSK-1292263 administrated at dose of 10 or 30 mg/kg or vehicle control at 2 hours prior to insulin infusion in hyperinsulinemic-euglycemic clamps stimulates glucagon secretion without increasing blood glucose levels Sprague-Dawley rats. ^[2]
• Clinical Trials: GSK1292263 has finished Phase II clinical trial for Diabetes Mellitus, Type 2.

Protocol

• Protocol: Animal Study ^[2]
• Animal Models: male Sprague-Dawley rats
• Formulation: 0.9% sodium chloride solution
• Doses: 3-30 mg/kg

References

• References: [1] Zhu X, et al. Eur J Med Chem, 2011, 46(7), 2901-2907.
• References: [2] Brown KK, et al. Diabetes, 2010, 59(Suppl. 1), Abst 1733-P.

参考文献

• Zhu X, et al. Eur J Med Chem, 2011, 46(7), 2901-2907.
• Brown KK, et al. Diabetes, 2010, 59(Suppl. 1), Abst 1733-P.