CAS NO: | 1032823-75-8 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
10mg | 电议 |
50mg | 电议 |
200mg | 电议 |
Cas No. | 1032823-75-8 |
化学名 | 5-[4-[[6-(4-methylsulfonylphenyl)pyridin-3-yl]oxymethyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole |
Canonical SMILES | CC(C)C1=NOC(=N1)N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(=O)(=O)C |
分子式 | C23H28N4O4S |
分子量 | 456.56 |
溶解度 | ≥ 21.1mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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. References: |