AMG 487 (C09-0735-593)

InformationAMG 487 AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.TargetsCXCR3-CXCL10 (Cell-free assay); CXCR3-CXCL11 (Cell-free assay) 8.0 nM; 8.2 nMIn vitroAMG487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle. AMG487 significantly affects DC maturity in vitro and function leading to impaired T cell activation, inducing DCs to have characteristics similar to tolerogenic DCs. AMG487 may directly play an immunomodulatory role during DC development and functional shaping.In vivoAMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA).Cell Research(from reference)Cell lines：Murine bone marrow-derived DCs (BMDCs) Concentrations：3 μM, 15 μM, 30 μM, 60 μM Incubation Time：over 6 days. Specifications and Purity: 98%. Molecular Formula: C32H28F3N5O4. Molecular Weight: 603.59. PubChem CID: 24957182. Isomeric SMILES: CCOC1=CC=C(C=C1)N2C(=O)C3=C(N=CC=C3)N=C2[C@@H](C)N(CC4=CN=CC=C4)C(=O)CC5=CC=C(C=C5)OC(F)(F)F.