Bay 41-4109 racemate
产品说明书
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同义名 : | (±)-BAY 41-4109; BAY41-4109 Racemic |
| CAS号 : | 298708-79-9 | |
| 货号 : | A127980 | |
| 分子式 : | C18H13ClF3N3O2 | |
| 纯度 : | 99% | |
| 分子量 : | 395.76 | |
| MDL号 : | MFCD30729326 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Human hepatitis B virus (HBV) causes a communicable disease that spreads worldwide and has brought about considerable economic losses due to human mortality and morbidity[3]. BAY 41-4109 racemate is the racemate of BAY 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM[4]. 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[5]. 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[6]. BAY 41-4109 dose-dependently reduces viral DNA in the liver and plasma with efficacy comparable to 3TC. It also 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[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.53mL 0.51mL 0.25mL |
12.63mL 2.53mL 1.26mL |
25.27mL 5.05mL 2.53mL |
| 参考文献 |
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