Bay 41-4109

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的非核苷类 HBV 核衣壳成熟抑制剂，IC50 为 0.05 uM。

A potent, non-nucleosidic inhibitor of HBV nucleocapsid maturation with IC50 of 0.05 uM; reduces HBV core protein levels in cell culture, possess in vitro and in vivo antiviral activity. HBV infection Discontinued.

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.

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.

Bay-414109

Microbiology/Virology

HBV

HBV

Infection

HBV Infection

298708-81-3

395.7629

C18H13ClF3N3O2

>98% (HPLC)

DMSO: ≥ 44 mg/mL

O=C(C1=C(C)NC(C2=NC=C(F)C=C2F)=N[C@H]1C3=CC=C(F)C=C3Cl)OC

5-Pyrimidinecarboxylic acid, 4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoro-2-pyridinyl)-1,4-dihydro-6-methyl-, methyl ester, (4R)-

(-20℃)

With Ice Pack

≥ 2 years