GW 9508

An agonist of GPR40

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

347.4

≥98%

OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1

C22H21NO3

885101-89-3

≥ 4 years

DMF: 20 mg/ml DMSO: 15 mg/ml Ethanol: 20 mg/ml Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml Methanol: 30 mg/ml

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. British Journal of Pharmacology 148, 619-628 (2006).

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