GLPG0974

GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43, IC50 = 9 nM). It is selective for FFAR2 over FFAR3 at concentrations up to 30 µM and over a panel of 55 receptors, ion channels, and transporters at 10 µM. GLPG0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM). GLPG0974 also inhibits a human FFAR2-based designer receptor exclusively activated by designer drugs (hFFAR2-DREADD, IC50 = 36.31 nM in a cell-based beta-arrestin-2 recruitment assay). It inhibits glucagon-like peptide 1 (GLP-1) secretion induced by the hFFA2-DREADD ligand sorbic acid in isolated colonic crypts from mice expressing hemagglutinin-tagged hFFAR2-DREADD when used at a concentration of 10 µM.Formal Name: 4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]-butanoic acid. CAS Number: 1391076-61-1. Molecular Formula: C25H25ClN2O4S. Formula Weight: 485.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Ethanol: Soluble. SMILES: O=C(N1CC[C@]1(C)C(N(CC2=CC(Cl)=CC=C2)CCCC(O)=O)=O)C3=CSC4=C3C=CC=C4. InChi Code: InChI=1S/C25H25ClN2O4S/c1-25(11-13-28(25)23(31)20-16-33-21-9-3-2-8-19(20)21)24(32)27(12-5-10-22(29)30)15-17-6-4-7-18(26)14-17/h2-4,6-9,14,16H,5,10-13,15H2,1H3,(H,29,30)/t25-/m1/s1. InChi Key: MPMKMQHJHDHPBE-RUZDIDTESA-N.