In vitro
Vicriviroc is nearly 6-fold less active than SCH-C (IC50 = 5.8 uM versus 1.1 uM) in attenuating hERG current among voltage-clamped L929 cells, indicating a reduced potential for cardiac effects. Vicriviroc inhibits MIP-1alpha induced migration of Ba/F3 cells stably expressing recombinant human CCR5, with IC50 of 0.91 nM. Vicriviroc is also highly active against a Clade G Russian isolate RU570 with EC90 of 16 nM, which is resistant to inhibition by SCH-C (EC90 > 1 uM). Vicriviroc could target an early step in the viral life cycle prior to reverse transcription and virion maturation, the targets of reverse transcriptase inhibitor and protease inhibitor, respectively.
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