| Bioactivity | Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell. | ||||||||||||
| Target | EC50：3.75 nM (anti-HBV, HepG2 cell) | ||||||||||||
| Invitro | Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) has a EC50 of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses[1].Entecavir monohydrate is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2]. | ||||||||||||
| In Vivo | Daily oral treatment with Entecavir monohydrate at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks[3]. | ||||||||||||
| Name | Entecavir monohydrate | ||||||||||||
| CAS | 209216-23-9 | ||||||||||||
| Formula | C12H17N5O4 | ||||||||||||
| Molar Mass | 295.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997 Jul;41(7):1444-8. [2]. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56. [3]. Genovesi EV, et al. Efficacy of the carbocyclic 2'-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17. |
Entecavir monohydrate
CAS: 209216-23-9 F: C12H17N5O4 W: 295.29
Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an E
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