AMG 487

AMG 487 is a chemokine (C-X-C motif) receptor 3 (CXCR3) antagonist (IC50 = 8.2 nM in a radioligand binding assay). It inhibits cell migration induced by chemokine (C-X-C motif) ligand 10 (CXCL10), CXCL11, and CXCL9 (IC50s = 8, 15, and 36 nM, respectively). In vivo, AMG 487 (3 mg/kg) inhibits bronchoalveolar lavage fluid (BALF) cell infiltration in a mouse model of bleomycin-induced cellular recruitment. It reduces the number of lung metastases in the K7M2 and Saos-LM7 osteosarcoma mouse xenograft models. AMG 487 (5 mg/kg) also restores mitochondrial function and inhibits mitochondrial-dependent hepatocellular apoptosis in a mouse model of non-alcoholic steatohepatitis (NASH).Formal Name: N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)-benzeneacetamide. CAS Number: 473719-41-4. Molecular Formula: C32H28F3N5O4. Formula Weight: 603.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 60 mg/ml. lambdamax: 269 nm. SMILES: O=C(N([C@@H](C1=NC(N=CC=C2)=C2C(N1C3=CC=C(OCC)C=C3)=O)C)CC4=CN=CC=C4)CC5=CC=C(OC(F)(F)F)C=C5. InChi Code: InChI=1S/C32H28F3N5O4/c1-3-43-25-14-10-24(11-15-25)40-30(38-29-27(31(40)42)7-5-17-37-29)21(2)39(20-23-6-4-16-36-19-23)28(41)18-22-8-12-26(13-9-22)44-32(33,34)35/h4-17,19,21H,3,18,20H2,1-2H3/t21-/m1/s1. InChi Key: WQTKNBPCJKRYPA-OAQYLSRUSA-N.