| 產品描述： | BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM |
| 靶點： |
IC50&Target: 53 nM (HBV);HBV |
| 體外研究： |
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 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 |
| 體內研究： |
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 |
| 參考文獻： |
1. Weber O, et al. Inhibition of human hepatitis B virus (HBV) by a novel non-nucleosidic compound in a transgenic mouse model. Antiviral Res. 2002 May;54(2):69-78. 2. Stray SJ, et al. BAY 41-4109 has multiple effects on Hepatitis B virus capsid assembly. J Mol Recognit. 2006 Nov-Dec;19(6):542-8. 3. Wu GY, et al. Inhibition of hepatitis B virus replication by Bay 41-4109 and its association with nucleocapsid disassembly. J Chemother. 2008 Aug;20(4):458-67. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.527 ml |
12.634 ml |
25.268 ml |
| 5 mM |
0.505 ml |
2.527 ml |
5.054 ml |
| 10 mM |
0.253 ml |
1.263 ml |
2.527 ml |
| 50 mM |
0.051 ml |
0.253 ml |
0.505 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京