GW 9508

GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC₅₀ = 47.8 nM for calcium mobilization in HEK293 cells).¹ It is selective for GPR40/FFA1 over GPR120/FFA4 (EC₅₀ = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC₅₀s = >50 µM).¹ GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.¹ It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.²

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1. Briscoe, C.P., Peat, A.J., McKeown, S.C., 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. 148(5), 619-628 (2006).

2. Li, M., Meng, X., Xu, J., et al. GPR40 agonist ameliorates liver X receptor-induced lipid accumulation in liver by activating AMPK pathway. Sci. Rep. 6:25237, (2016).

Huan, Y., Jiang, Q., Li, G., et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci. Rep. 7(1), 4351 (2017).