298708-79-9
298708-79-9 结构式
基本信息
Bay 41-4109 (racemate)
BAY41-4109 RACEMATE
BAY-41-4109 RACEMATE
Methyl 4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoropyridin-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate
5-Pyrimidinecarboxylic acid, 4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoro-2-pyridinyl)-1,4-dihydro-6-methyl-, methyl ester
4-?(2-Chloro-?4-?fluorophenyl)?-?2-?(3,?5-?difluoro-?2-?pyridinyl)?-?1,?4-?dihydro-?6-?methyl-?5-?pyrimidinecarboxylic Acid Methyl Ester
物理化学性质
Ethanol:11.0(Max Conc. mg/mL);27.79(Max Conc. mM)
常见问题列表
| Target | Value |
|
HBV capsid
(Cell-free assay) | 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. BAY 41-4109 is equally effective at inhibiting HBV DNA release and the cytoplasmic HBcAg level, with IC 50 s 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.
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.