产品描述:
GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} 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.{14194} 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.{43588}