|
| | GSK1292263 Basic information |
| Product Name: | GSK1292263 | | Synonyms: | CS-417;GPR119 receptor agonist GS1292263;3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-;5-[[[1-[3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methyl]oxy]-2-[4-(methylsulfonyl)phenyl]pyridine;3-isopropyl-5-(4-(((6-(4-(Methylsulfonyl)phenyl)pyridin-3-yl)oxy)Methyl)piperidin-1-yl)-1,2,4-oxadiazole;3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxa;GSK1292263;5-((1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methoxy)-2-(4-(methylsulfonyl)phenyl)pyridine | | CAS: | 1032823-75-8 | | MF: | C23H28N4O4S | | MW: | 456.56 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1032823-75-8.mol |  |
| | GSK1292263 Chemical Properties |
| Boiling point | 655.1±65.0 °C(Predicted) | | density | 1.23 | | storage temp. | Store at -20°C | | solubility | ≥21.1 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | 4.75±0.32(Predicted) |
| | GSK1292263 Usage And Synthesis |
| Biological Activity | gsk1292263 is a novel agonist of gpr119 receptor agonist and is used for the treatment of type 2 diabetes.gpr119 is described as a class a (rhodopsin-type) orphan gpcr with no close primary sequence relative in the human genome. the activation of gpr119 increases the intracellular accumulation of camp, resulting in enhanced insulin secretion from pancreatic β-cells and increased release of the gut peptides glp-1 (glucagon-like peptide 1), gip (glucose-dependent insulinotropic peptide) and pyy (polypeptide yy).in vitro, gsk1292263 treatment displayed little inhibition towards cyps (cyp1a2, 2c9, 2c19, 2d6, 3a4), p-gp, oatp1b3, or oct2. however, gsk1292263 inhibited bcrp and oatp1b1, which are transporters involved in statin disposition 1.in the glucose tolerance test in rats, administration of gsk-1292263 significantly increases the peak insulin response and insulin auc (0-15 min) as compared with the values in the vehicle control. the upregulation of insulin was found to correlate with an increase in the glucose disposal rate. in hyperinsulinemic-euglycemic clamps, gsk-1292263 administration on sprague-dawley rats at dose of 10 or 30 mg/kg 2 hours prior to insulin infusion can promote glucagon secretion with no increase of blood glucose levels 2. | | target | GPR119 | | references | 1. polli jw, hussey e, bush m, et al. evaluation of drug interactions of gsk1292263 (a gpr119 agonist) with statins: from in vitro data to clinical study design. xenobiotica; the fate of foreign compounds in biological systems. 2013;43(6):498-508.2. zhu x, huang d, lan x, et al. the first pharmacophore model for potent g protein-coupled receptor 119 agonist. european journal of medicinal chemistry. 2011;46(7):2901-2907. |
| | GSK1292263 Preparation Products And Raw materials |
|
