产品描述:
GPR40 (free fatty acid receptor 1; FFAR1) is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120 (FFAR4), another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid.{14194} In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.{14194}