GSK1292263 Inhibitor CAS No. 1032823-75-8

Cat. No.	Name	Size	Price
KI1192	GSK1292263	10 mg	$608
	GSK1292263	50 mg	$1568
	GSK1292263	200 mg	$3968

Chemical Characteristic

Product Name	GSK1292263
Synonyms	GSK263
CAS No.	1032823-75-8
Molecular Weight	456.56
Formula	C₂₃H₂₈N₄O₄S
Chemical Name	5-[[[1-[3-(1-Methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl]methyl]oxy]-2-[4-(methylsulfonyl)phenyl]pyridine
Smiles	c1(ccc(cn1)OCC1CCN(CC1)c1onc(n1)C(C)C)c1ccc(cc1)S(=O)(=O)C
Chemical Structure

Biological activities

GSK1292263 is a novel GPR119 agonist. GSK1292263 increases fasting plasma high-density lipoprotein cholesterol (HDLc). GSK1292263 reduces fasting LDLc, as well as fasting and prandial triglycerides. GSK1292263 interacts with CYP3A4, resulting in inhibition atorvastatin metabolism by 32% at 100 µM. GSK1292263 at the dose of 3 µM inhibits BCRP-mediated transport of [³H]cimetidine by 52% inhibition. GSK1292263 inhibits OATP1B1 by inhibition of 40% at 3 µM. In addition, GSK1292263 inhibits OCT1 transport by 69% and OCT2 by 26% at 30 µM. Combination of GSK1292263 with rosuvastatin increases the rosuvastatin AUC_{(0-inf) and C_{max by ~40% relative to rosuvastatin administered alone. ^[1] In a 6-week study performed in Zucker diabetic fatty rats, GSK-1292263 statistically and significantly increases insulin immunoreactivity in pancreatic sections.^[2] GSK1292263 improves glucose regulation in animal models of diabetes. However, GSK1292263 doesn?? affect plasma glucose in type 2 diabetics.^[3]}}

References

[1] Polli JW, et al. Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: from in vitro data to clinical study design. Xenobiotica. 2012. [2] Preclinical and first-in-human data reported on GSK-1292263 for type 2 diabetes [3] Nunez DJ, et al. Novel and profound lipid effects of GSK1292263, a potent and selective GPR119 agonist, in dyslipidemic subjects. Circulation. 2012, 126: A9918.

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