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GSK1292263 1032823-75-8

更新时间:2024-02-02

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GSK1292263 1032823-75-8
上海一基实业有限公司是主要从事、配套试剂的生产和销售的企业,产品用途:科研实验,标准对照品研究中心代理的作为一种衡量标准。

GSK1292263  1032823-75-8

GSK-1292263
分子式:C23H28N4O4S   分子量:456.56
 
产品描述
GSK-1292263是新型GPR119 激动剂,用于治疗2型糖尿病。
靶点
GPR119
         
IC50
           
体外研究
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. 
体内研究
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.
溶解性
DMSO 34 mg/mL,水 <1 mg/mL,乙醇 <1 mg/mL
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO

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