| Identification | Back Directory | [Name]
GSK1292263 | [CAS]
1032823-75-8 | [Synonyms]
CS-417
GSK1292263
GSK1292263 USP/EP/BP
GSK-1292263;GSK 1292263
GPR119 receptor agonist GS1292263
3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-
3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxa
5-((1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methoxy)-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
Pyridine, 5-[[1-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methoxy]-2-[4-(methylsulfonyl)phenyl]-
5-[[[1-[3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methyl]oxy]-2-[4-(methylsulfonyl)phenyl]pyridine
5-[[[1-[3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methyl]oxy]-2-[4-(methylsulfonyl)phenyl]pyridine gsk 1292263 | [Molecular Formula]
C23H28N4O4S | [MDL Number]
MFCD18385004 | [MOL File]
1032823-75-8.mol | [Molecular Weight]
456.558 |
| Chemical Properties | Back Directory | [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) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. |
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