CAS No. : 1032823-75-8

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000196
Molecular Formula:C23H28N4O4S
Molecular Weight:456.56
Target:Free Fatty Acid Receptors
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Appearance:Solid powder
Purity: > 98%
Cat No:I000196
Cas No:1032823-75-8

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.
IC50 value:
Target: 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].

1:Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies. Nunez DJ, Bush MA, Collins DA, McMullen SL, Gillmor D, Apseloff G, Atiee G, Corsino L, Morrow L, Feldman PL.PLoS One. 2014 Apr 3;9(4):e92494. doi: 10.1371/journal.pone.0092494. eCollection 2014. PMID: 24699248 Free PMC Article
2:Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: from in vitro data to clinical study design. Polli JW, Hussey E, Bush M, Generaux G, Smith G, Collins D, McMullen S, Turner N, Nunez DJ.Xenobiotica. 2013 Jun;43(6):498-508. doi: 10.3109/00498254.2012.739719. Epub 2012 Dec 21. PMID: 23256625
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