Ancriviroc (SCH-351125) is an orally active CCR5 antagonist with an IC 50 value of 13 nM against hCCR5 . Ancriviroc specifically binds to hCCR5, blocks ligand-induced signal transduction, calcium influx, GTPγS binding, chemotaxis, ligand binding, and HIV-1 entry, induces conformational changes in CCR5 , and inhibits infection and replication of R5-tropic HIV-1 .
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