1286279-29-5

BMS 813160 is a dual antagonist of chemokine receptor 2 (CCR2) and CCR5 (IC₅₀s = 6.2 and 3.6 nM, respectively, in radioligand binding assays). It inhibits chemotaxis induced by the CCR2 ligand MCP-1 in THP-1 cells the CCR5 ligand MIP-1β in isolated peripheral T cells with IC₅₀ values of 0.8 and 1.1 nM, respectively. BMS 813160 inhibits peritoneal monocyte and macrophage infiltration in an hCCR-2 KI mouse model of thioglycolate-induced peritonitis, with 54% inhibition when administered at a dose of 50 mg/kg twice per day.

BMS-813160, a dual CCR2/CCR5 chemokine antagonist.

CCR5: 3.6 nM (IC₅₀); CCR2: 6.2 nM (IC₅₀)

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[1] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[2] NORMAN P. A dual CCR2/CCR5 chemokine antagonist, BMS-813160? Evaluation of WO2011046916.[J]. Expert Opinion on Therapeutic Patents, 2011, 21 12: 1919-1924. DOI: 10.1517/13543776.2011.622750