BAY 41-4109 racemate是BAY 41-4109的消旋体。BAY 41-4109有效抑制人乙型肝炎病毒，IC50值为53 nM。

BAY 41-4109 racemate is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.

BAY 41-4109 is able to both accelerate and misdirect capsid assembly in vitro. BAY 41-4109 stabilized the preformed capsids, up to a ratio of one inhibitor molecule per two dimers[2]. 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[3]..

BAY 41-4109 reduces viral DNA in the liver and in the plasma in a dose-dependent manner 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[1].BAY41-4109 inhibits virus production in vivo by a mechanism that targets the viral capsid[2].

Cellular metabolism is evaluated by MTT colorimetry. HepG2.2.15 cells are plated at a density of 2 × 103 cells per well in 96-well plates. After 8 d of treatment with different concentrations of each antiviral compound, 20 μL of MTT solution (5 g/L) are added to each well and incubated at 37°C for 4 h. Next, 150 μL of DMSO is added and stirred for 10 min to dissolve the crystals. Absorbance values are recorded at 490 nm by using an ELISA reader. The MTT values are calculated using the curve regression equation[3].

298708-79-9

C18H13ClF3N3O2

395.77

DMSO:28 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years