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网站主页 化工产品目录 生物化工 抑制剂 内分泌及激素(Endocrinology & Hormones) GPR 激动剂 GSK1292263
  • GSK1292263

GSK1292263

GSK1292263
1032823-75-8
￥1605.01 10mg/50mg 起订
其他 更新日期：2020-01-16

Selleck中国

非会员
联系人：Selleck中国
电话：021-68591985拨打
邮箱：info@selleck.cn

产品详情:

英文名称：
GSK1292263
CAS号：
1032823-75-8
规格：
10mg/50mg
货号：
S2149
Selleck Chemicals美国品牌，中国库存现货，GPR抑制剂，CAS#1032823-75-8。
更多详情请访问中国唯一官方网站： http://www.selleck.cn/products/GSK1292263.html


生物活性

产品描述 GSK-1292263是一种新型GPR119激动剂，用于治疗2型糖尿病。Phase 2。
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. 

[1]
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. 

[2]
临床实验 GSK1292263 has finished Phase II clinical trial for Diabetes Mellitus, Type 2.
特征  

动物实验: 

[2]

动物模型 male Sprague-Dawley rats
配制 0.9% sodium chloride solution
剂量 3-30 mg/kg
温馨提示：不可用于临床治疗。
GSK1292263;化学试剂

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