2015年6月1日星期一

GSK1292263|GPR119 receptor agonist|DC Chemicals

GSK1292263|GPR119 receptor agonist|DC Chemicals
GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

Catlog: DC8117| Product name: GSK1292263| Cas: 1032823-75-8| Other names: GSK-1292263,GSK 1292263| Molecule Formula: C23H28N4O4S| MW: 456.56. Purity: >98%

Price: 100mg: 700 USD; 250mg: 1400 USD; 1000mg: 2500 USD

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.
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.
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.

For research and scientific purpose only, not for human use.

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