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RO-9187
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RO-9187
CAS No. : 876708-03-1
MCE 站:RO-9187
产品活性:RO-9187是高效的HCV病毒复制抑制剂,IC50值为171 nM。
研究领域:Anti-infection
作用靶点:HCV
In Vitro: RO-9187 is excellent substrates for deoxycytidine kinase and is phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. RO-9187 inhibits RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations with similar potencies, suggesting no cross-resistance with either R1479 (4′-azidocytidine) or 2′-C-methyl nucleosides. The formation of RO-9187-TP increased in a time- and dose-dependent manner. The maximal triphosphate concentration at 24 h is 87 pmol/106 cells with half-maximal triphosphate formation achieved at 12 μM RO-9187.
In Vivo: Plasma exposures of RO-9187 in rats increase in a dose-dependent manner between 10 and 2000 mg/kg after oral dosing. Plasma concentrations of 1.4 and 26 μM (390 and 7454 ng/mL) are achieved in rats and dogs at the 10 mg/kg dose level, respectively. Plasma concentrations up to 57 μM are achieved in rats dosed with 2000 mg/kg/day.
相关产品:Natural Product Like Compound Library | Bioactive Compound Library Plus | Anti-Infection Compound Library | Antiviral Compound Library | Nucleotide Compound Library | Anti-Hepatitis C Virus Compound Library | Resiquimod | Honokiol | Ribavirin | Deferiprone | U18666A | AG-1478 | EIDD-1931 | Artemisinin | NIM811 | Alisporivir | Myriocin | Mizoribine | Merimepodib | NHC-triphosphate | PSI-7409 | Peretinoin | BLT-1 | Celgosivir hydrochloride | Clemizole hydrochloride | Gentiopicroside | NM107 | ITX5061 | Deapioplatycodin D | KIN1408 | Oglufanide | PSI-6130 | RO8191 | Taribavirin hydrochloride
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