- GW9508
- GW-1100
- TUG-770
- TAK-875
| GSK1292263Novel GPR119 agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | GSK1292263 is a novel agonist of GPR119. | |||||
| Targets | GPR119 | |||||
| IC50 | ||||||
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| Cas No. | 1032823-75-8 | SDF | Download SDF |
| Chemical Name | 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 | ||
| Formula | C23H28N4O4S | M.Wt | 456.56 |
| Solubility | ≥21.1mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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: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.
