GW 1100

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. 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.Formal Name: 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-benzoic acid, ethyl ester. CAS Number: 306974-70-9. Molecular Formula: C27H25FN4O4S. Formula Weight: 520.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml, DMSO: 2 mg/ml. lambdamax: 243 nm. SMILES: FC1=CC=C(CSC(N(C2=CC=C(C(OCC)=O)C=C2)C=C3CC4=CN=C(OCC)N=C4)=NC3=O)C=C1. InChi Code: InChI=1S/C27H25FN4O4S/c1-3-35-25(34)20-7-11-23(12-8-20)32-16-21(13-19-14-29-26(30-15-19)36-4-2)24(33)31-27(32)37-17-18-5-9-22(28)10-6-18/h5-12,14-16H,3-4,13,17H2,1-2H3. InChi Key: PTPNCCWOTBBVJR-UHFFFAOYSA-N.