GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. The predicted EC50 of GSK1292263 against GPR119 in vitro is at the nanomolar range. (1) The GPR119 receptor is a GPCR which is selectively expressed on pancreatic beta cells and intestinal enteroendocrine cells. Agonists to GPR119 stimulate glucose-dependent insulin secretion in vitro and lower an elevated blood glucose level in vivo.(2)
In vivo, GSK1292263 treatment significantly increases in the peak insulin response and insulin AUC(0-15 min) by 30-60% compared with vehicle control in the intravenous glucose tolerance test. This insulin upregulation correlated with a significant increase in the glucose disposal rate. (3)
Technical information:
| Chemical Formula: | C23H28N4O4S | |
| CAS #: | 1032823-75-8 | |
| Molecular Weight: | 456.56 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | 3-isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxadiazole | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | GSK1292263, GSK 1292263, GSK-1292263 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Zhu X et al., The first pharmacophore model for potent G protein-coupled receptor 119 agonist. Eur J Med Chem. 2011, 46(7):2901-7 Pubmed ID: 21524831 |
| 2. | Overton HA, et al., GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity. Br J Pharmacol. 2008, 153 Suppl 1:S76-81. Pubmed ID: 18037923 |
| 3. | Brown, K.K. et al. Diabetes [70th Annu Meet Sci Sess Am Diabetes Assoc (ADA) (June 25-29, Orlando) 2010] 2010, 59(Suppl. 1): Abst 407 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
