599179-03-0

Vicriviroc is a chemokine (C-C motif) receptor 5 (CCR5) antagonist (K_i = 2.5 nM). It selectively inhibits CCR5 over M₁ and M₂ muscarinic acetylcholine receptors (K_is = >10,000 nM for both) and human-ether-a-go-go (hERG) potassium channels (IC₅₀ = 5.8 μM). Vicriviroc decreases chemotaxis induced by chemokine (C-C motif) ligand 3 (CCL3) in Ba/F3 cells expressing recombinant human CCR5 with an IC₅₀ value of 0.91 nM. It inhibits the replication of 30 R5-tropic HIV-1 clinical isolates in peripheral blood mononuclear cells (PBMCs; EC₅₀s = 0.04-1.4 nM) and reduces viral entry of seven drug-resistant strains of HIV-1 in U87 cells expressing CD4 and CCR5 (EC₅₀s = 8.7-32.9 nM).

Antiviral, CCR5 antagonist, treatment of autoimmune conditions.

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