TMC647055 Choline salt 是一种细胞渗透性的, 选择性HCV NS5B抑制剂, 评估病毒RdRp引物依赖性转录测定中, 平均IC50为34 nM。
TMC647055 choline salt is a cell-permeating, selective HCV NS5B inhibitor, eliciting a mean IC50 of 34 nM, as assessed in the RdRp primer-dependent transcription assay.IC50 value: 34 nM [1]Target: HCV NS5Bin vitro: TMC647055 is a novel and potent nonnucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase. TMC647055 shows high selectivity for HCV when evaluated with a broad panel of human DNA and RNA viruses. TMC647055 shows median EC50 changes in the replicon assay of 9-, 3-, and 371-fold for L392I, V494A, and P495L, respectively, The median EC50 of TMC647055 on NS5B sequences derived from clinical isolates of genotypes 1a, 1b, 3a, 4a, and 6a ranged between 27 nM and 113 nM.[1]
[1]. Devogelaere B, et al. TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage. Antimicrob Agents Chemother. 2012 Sep;56(9):4676-4684.
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