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Bay 41-4109 racemate

CAS No. : 298708-79-9

MCE 站：Bay 41-4109 racemate

产品活性：BAY 41-4109 racemate是BAY 41-4109的消旋体。BAY 41-4109是人乙型肝炎病毒HBV的有效抑制剂，IC₅₀值为53 nM。

研究领域：Anti-infection

作用靶点：HBV

In Vitro: BAY 41-4109 is able to both accelerate and misdirect capsid assembly in vitro. Preformed capsids are stabilized by BAY 41-4109, up to a ratio of one inhibitor molecule per two dimers. BAY 41-4109 is equally effective at inhibiting HBV DNA release and the cytoplasmic HBcAg level, with IC₅₀s of 32.6 and 132 nM in HepG2.2.15 cells, respectively. HBV DNA and HBcAg are inhibited in a dose-dependent manner, indicating that the anti-HBV mechanisms are associated with and dependent on the rate of HBcAg inhibition.

In Vivo: BAY 41-4109 reduces viral DNA in the liver and in the plasma dose-dependently with efficacy comparable to 3TC. BAY 41 -4109 reduces hepatitis B virus core antigen (HBcAg) in livers of HBV-transgenic mice. Pharmacokinetic studies in mice have shown rapid absorption, a bioavailability of 30% and dose-proportional plasma concentrations, about 60% in rats and dogs.BAY41-4109 inhibits virus production in vivo by a mechanism that targets the viral capsid.

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