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GSK1292263

In stock
Catalog No.
A8439
Novel GPR119 agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$230.00
In stock
10mg
$140.00
In stock
50mg
$470.00
In stock
200mg
$1,410.00
In stock

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt456.56
Cas No.1032823-75-8
FormulaC23H28N4O4S
Solubility≥21.1mg/mL in DMSO
Chemical Name5-[4-[[6-(4-methylsulfonylphenyl)pyridin-3-yl]oxymethyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole
SDFDownload SDF
Canonical SMILESCC(C)C1=NOC(=N1)N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(=O)(=O)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Description GSK1292263 is a novel agonist of GPR119.
Targets GPR119          
IC50            

Quality Control

Quality Control & MSDS

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Chemical structure

GSK1292263