Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor ofHBV, with anEC₅₀of 3.75 nM in HepG2 cell.

EC50: 3.75 nM (anti-HBV, HepG2 cell)^[2]

BMS-200475 has a EC₅₀of 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 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].

Daily oral treatment with BMS-200475 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].

277.28

Solid

C₁₂H₁₅N₅O₃

142217-69-4

恩替卡韦

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 44 mg/mL(158.68 mM)

*"≥" means soluble, but saturation unknown.

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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。