GPR40 and GPR120 are G protein-coupled receptors (GPCR) that are activated by medium and long-chain fatty acids. In addition, there is evidence of a link between GPR40 and the ability of fatty acids to acutely potentiate insulin secretion. GW 9508 is a small-molecule agonist of GPR40 and GPR120. Stimulation of intracellular Ca2+ mobilization by GW 9508 in human embryonic kidney (HEK) 293 cells expressing GPR40 and GPR120 was observed with EC50 values of 47 nM and 2.2 µM, respectively.1 GW9508 dose dependently potentiates glucose-stimulated insulin secretion and the KCl-mediated increase in insulin secretion in MIN6 cells.1
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 Pharmacol148619-628(2006).
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OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1
Background Reading
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 Pharmacol148619-628(2006).
GW 9508 is available in the following screening
library: