AMG 837

AMG 837 is a partial agonist of free fatty acid receptor 1 (FFAR1/GPR40). It induces calcium mobilization in CHO cells expressing FFAR1/GPR40 but not FFAR2/GPR43, FFAR3/GPR41, or FFAR4/GPR120 (EC50s = 0.0135, >10, >10, and >10 µM, respectively). AMG 837 induces insulin secretion in MIN6 pancreatic beta-cells and isolated mouse islets (EC50s = 0.0048 and 0.142 µM, respectively). It decreases plasma glucose levels and increases plasma levels of insulin in Zucker fa/fa rats when administered at doses of 0.3, 1, and 3 mg/kg. AMG 837 (100 mg/kg) also decreases plasma glucose and increases plasma insulin levels in a mouse model of diabetes induced by a high-fat diet and streptozotocin (STZ, Cay-13104).Formal Name: betaS-1-propyn-1-yl-4-[[4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]methoxy]-benzenepropanoic acid. CAS Number: 865231-46-5. Molecular Formula: C26H21F3O3. Formula Weight: 438.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml, DMSO: 5 mg/ml. lambdamax: 253 nm. SMILES: OC(C[C@H](C#CC)C(C=C1)=CC=C1OCC2=CC(C3=CC=C(C(F)(F)F)C=C3)=CC=C2)=O. InChi Code: InChI=1S/C26H21F3O3/c1-2-4-21(16-25(30)31)20-9-13-24(14-10-20)32-17-18-5-3-6-22(15-18)19-7-11-23(12-8-19)26(27,28)29/h3,5-15,21H,16-17H2,1H3,(H,30,31)/t21-/m0/s1. InChi Key: ZOPNBMMVVZRSGH-NRFANRHFSA-N.