货号 | 13831-5mg |
描述 | Entecavir is a potent deoxyguanosine nucleoside analog with antiviral activity selective for hepadnaviruses (EC50 = 3.7 nM against the hepatitis B virus (HBV) in cultured 2.2.15 liver cells).1 In vitro, the active intracellular form of entecavir, entecavir triphosphate, demonstrates a higher binding affinity for HBV DNA polymerase than the natural guanosine triphosphate substrate and effectively inhibits HBV DNA replication at 3 stages in the replication pathway: priming, reverse transcription, and DNA-dependent DNA synthesis.2 The potential therapeutic benefits of entecavir have been demonstrated in woodchuck and duck models of HBV.3 Activity was confirmed in phase I/II preclinical studies and entecavir received approval from the U.S. Food and Drug Administration for the treatment of adults with chronic hepatitis B.4 |
别名 | Baraclude;BMS 200475;SQ 34,676; |
供应商 | Cayman |
应用文献 | |
1.Innaimo, S.F.,Seifer, M.,Bisacchi, G.S., et al. Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virus. Antimicrobial Agents and Chemotherapy 41(7), 1444-1448 (1997). 2.Seifer, M.,Hamatake, R.K.,Colonno, R.J., et al. In vitro inhibition of hepadnavirus polymerases by the triphosphates of BMS-200475 and lobucavir. Antimicrobial Agents and Chemotherapy 42(12), 3200-3208 (1998). 3.Marion, P.L.,Salazar, F.H.,Winters, M.A., et al. Potent efficacy of entecavir (BMS-200475) in a duck model of hepatitis B virus replication. Antimicrobial Agents and Chemotherapy 46(1), 82-88 (2002). 4.Keeffe, E.B. and Marcellin, P. New and emerging treatment of chronic hepatitis B. Clin.Gastroenterol.Hepatol. 5(3), 285-294 (2007). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 295.3 |
分子式 | C12H15N5O3 • H2O |
CAS号 | 209216-23-9 |
稳定性 | ≥ 2 years |
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