BMS-753426 is a potent, selective and orally bioavailable antagonist of CCR2 with binding IC50 of 2.7 nM, 30-fold selectivity over CCR5.
BMS-753426 potently inhibits chemotaxis of human peripheral blood mononuclear cells (hPBMCs) induced by 10 nM MCP-1 with IC50 of 0.8 nM.
BMS-753426 (1, 25, and 100 mg/kg, oral) inhibits 28%, 74%, and 78% of monocyte/macrophage influx, respectively, in hCCR2 knock-in (KI) mice, with EC50 of 3.9 nM.
BMS-753426 (25 mg/kg, BID) reduces clinical score, histological evaluation of the spinal cordexperimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis in hCCR2 KI mice.
