GW1100 (306974-70-9) is a selective antagonist of GPR40. GW1100 inhibits GRP40-mediated Ca2+ increases stimulated GW9508 (Cat.# 10-1108) or linoleic acid (pIC50 = 5.99 for either agonist).1 The effects of GPR40 activation on insulin secretion in cells are also blocked by the addition of GW1100. GW1100 does not influence calcium mobilization mediated by GPR120.
1) Brisco et al. (2006), Pharmacological regulation of insulin secretion in MIN6 cells through fatty acid receptor GPR40: identification of agonist and antagonist molecules; Br. J. Pharmacol., 148 619
2) Nagatake et al. (2018), The 17,18-Epoxytetraenoic acid-G protein-coupled receptor 40 axis amelioraters contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques; J. Allergy Clin. Immunol., 142 470 [Focus Biomolecules Citation]