GW9508

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Background

GW9508 is a selective agonist of GPR40 and 120 with pEC50 value of 7.32 ± 0.03 and 5.46 ± 0.09, respectively [1].GPR40/120 belongs to G protein-coupled receptors (GPCRs) family and is activated by free fatty acids. Mucosal inflammation induced the overexpression of GPR40, GPR120, and several inflammatory cytokines, with correlations between ileal concentrations of tumor necrosis factor (TNF)-α and GPR expression levels [2] [3].GW9508 is a GPR40/120 agonist and is different from the reported GPR40/120 agonist GW1100. When tested with HEK-293 (human embryonic kidney) cells expressing GPR40 or GRP120, GW9508 treatment increased intracellular Ca2+ concentration via activating GPR40/120 in a dose-dependent manner [1]. In rat pancreaticβ-cells, GW9508 treatment activated KATP channels which inhibited GSIS through agonist of GPR40 and GPR120 [4]. When tested with TNF-α treated rat L cells, administration of GW9508 increased the expression of GLP-2 via activating GPR40 and 120 [2].

[1].Briscoe, C.P., et al., Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol, 2006. 148(5): p. 619-28.
[2].Tsukahara, T., et al., Tumor necrosis factor alpha decreases glucagon-like peptide-2 expression by up-regulating G-protein-coupled receptor 120 in Crohn disease. Am J Pathol, 2015. 185(1): p. 185-96.
[3].Habib, A.M., et al., Co-localisation and secretion of glucagon-like peptide 1 and peptide YY from primary cultured human L cells. Diabetologia, 2013. 56(6): p. 1413-6.
[4].Zhao, Y.F., et al., GW9508 inhibits insulin secretion by activating ATP-sensitive potassium channels in rat pancreatic beta-cells. J Mol Endocrinol, 2013. 51(1): p. 69-77.