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- Clevudine 163252-36-6

- Clevudine 163252-36-6
Clevudine 163252-36-6
产品描述 描述 Clevudine is an antiviral drug for the treatment of hepatitis B.纯度 98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 可溶性/溶解性 DMSO:52 mg/mL (199.83 mM)生物活性 靶点 RNA polymerase,DNA polymeraseIn vitro(体外研究) Clevudine is a potent antiviral agent against HBV (EC50 0.1 μM in HepG2 2.2.15 cells) as well as EBV, which has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. Clevudine is known to act specifically on viral DNA synthesis, and its triphosphate inhibits the HBV DNA synthesis in a dose-dependent manner without being incorporated into the DNA or chain termination. Clevudine results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Clevudine monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine.In vivo(体内研究) Clevudine is a potent antiviral agent against HBV (EC50 0.1 μM in HepG2 2.2.15 cells) as well as EBV, which has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. Clevudine is known to act specifically on viral DNA synthesis, and its triphosphate inhibits the HBV DNA synthesis in a dose-dependent manner without being incorporated into the DNA or chain termination. Clevudine results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Clevudine monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine.参考文献 参考文献 1. Chong Y, et al. Bioorg Med Chem Lett, 2002, 12(23), 3459-3462.
2. Hu R, et al. Antimicrob Agents Chemother, 2005, 49(5), 2044-2049.
研究领域 研究领域 MetabolismTypes of diseaseDrug DiscoverySmall Molecule DrugLead Compound DiscoveryClevudine 163252-36-6温馨提示:本产品仅作科研实验使用,不支持临床等研究
