CAS No. : 209216-23-9
(Synonyms: BMS200475 (monohydrate); SQ34676 (monohydrate))
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| Cat. No. : | HY-13623A |
| M.Wt: | 295.29 |
| Formula: | C12H17N5O4 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 50 mg/mL;H2O : 2.8 mg/mL (ultrasonic;warming) |
Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
IC50 & Target:EC50:3.75 nM (anti-HBV, HepG2 cell)[1]
In Vitro: 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].
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