Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent HBV inhibitor (IC50: 53 nM).

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 [2]. In HepG2.2.15 cells, BAY 41-4109 is equally effective at inhibiting HBV DNA release and the cytoplasmic HBcAg level (IC50s: 32.6 and 132 nM). HBV DNA and HBcAg are inhibited in a dose-dependent manner [3].

BAY 41-4109 reduces viral DNA in the liver and in the plasma dose-dependently with efficacy comparable to 3TC. BAY 41 -4109 reduces the 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 [1]. BAY41-4109 inhibits virus production in vivo by a mechanism that targets the viral capsid [2].

476617-51-3

C18H13ClF3N3O2

395.76

DMSO:37 mg/mL (93.49 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years