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476617-51-3

中文名称 476617-51-3
英文名称 Bay 41-4109 (less active enantiomer)
CAS 476617-51-3
分子式 C18H13ClF3N3O2
分子量 395.76
MOL 文件 476617-51-3.mol
476617-51-3 结构式 476617-51-3 结构式

基本信息

英文别名
Bay 41-4109 (less active enantiomer)
Bayer 41-4109 less active enantiomer
BAY41-4109 LESS ACTIVE ENANTIOMER
BAY-41-4109 LESS ACTIVE ENANTIOMER
BAYER 41-4109 LESS ACTIVE ENANTIOMER
methyl (4S)-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, (4S)-

物理化学性质

储存条件-20°C储存
溶解度DMSO : ≥ 37 mg/mL (93.49 mM)
形态Solid
颜色Light yellow to yellow
476617-51-3价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2023/03/20HY-100029B476617-51-3
Bay 41-4109 (less active enantiomer)
476617-51-310mM * 1mLin DMSO2873元
2023/03/20HY-100029B476617-51-3
Bay 41-4109 (less active enantiomer)
476617-51-35mg3300元
2023/03/20HY-100029B476617-51-3
Bay 41-4109 (less active enantiomer)
476617-51-310mg5000元

常见问题列表

生物活性
Bay 41-4109 less active enantiomer 是比BAY 41-4109活性低的对应体。BAY 41-4109是人乙型肝炎病毒HBV的有效抑制剂,IC50值为53 nM。
靶点

IC50: 53 nM (HBV, Bay 41-4109)

体外研究

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.

体内研究

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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