AMG 487 (CAS 473719-41-4) is a selective small molecule antagonist targeting chemokine receptor CXCR3 a G protein-coupled receptor involved in immune cell migration It competitively inhibits CXCR3 binding to its cognate chemokines including IP-10 and ITAC with IC50 values reported at approximately 8 nM and 8 2 nM respectively Cell-based assays indicate AMG 487 can effectively impede IP-10 ITAC and MIG-mediated chemotaxis and ITAC-induced calcium mobilization AMG 487 is metabolized via CYP3A4 and CYP3A5 to metabolites one of which (M2) inhibits CYP3A Given these characteristics AMG 487 provides a valuable pharmacological tool for investigating CXCR3 functions in inflammatory and immunological research