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中文名称: Bay 41-4109 (less active enantiomer)
英文名称: Bay 41-4109 (less active enantiomer)
CAS No: 476617-51-3
分子式: C18H13ClF3N3O2
分子量: 395.76
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
B10580 Bay 41-4109 (less active enantiomer) (psaitong)
包装规格：
5mg in glass bottle
溶解性：
溶于DMSO（≥ 37 mg/mL)
产品描述：

基本信息

产品编号：B10580

产品名称：Bay 41-4109 (less active enantiomer)

CAS:

476617-51-3

 

储存条件

粉末

-20℃

四年

 

 

分子式：

C18H13ClF3N3O2

溶于液体

-80℃

六个月

分子量

395.76

-20℃

一个月

化学名： 

methyl (4S)-4-(2-chloro-4-fluorophenyl)-2-(3,5-difluoropyridin-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate

 

Solubility (25°C)

 

体外

DMSO

≥30mg/mL (75.80mM)

Ethanol

 

Water

 

体内

现配现用

 

＜1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.5268mL

12.6339mL

25.2678mL

5mM

0.5054mL

2.5268mL

5.0536mL

10mM

0.2527mL

1.2634mL

2.5268mL

 

生物活性

产品描述

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53nM。

靶点/IC50

HBV, Bay 41-4109

IC50: 53nM

 

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 IC50s of 32.6 and 132nM 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.

 

推荐实验方法(仅供参考)

细胞实验:

 

Cell Assay

Cellular metabolism is evaluated by MTT colorimetry. HepG2.2.15 cells are plated at a density of 2×103 cells per well in 96- well plates. After 8 d of treatment with different concentrations of each antiviral compound, 20μL of MTT solution (5 g/L) are added to each well and incubated at 37°C for 4 h. Next, 150μL of DMSO is added and stirred for 10 min to dissolve the crystals. Absorbance values are recorded at 490nm by using an ELISA reader. The MTT values are calculated using the curve regression equation.

 

 

动物实验:

 

Animal Administration

Mice: The HBV-transgenic mice are used in the study. Compounds (BAY 41-4109) are formulated as a suspension in 0.5% Tylose and administered per os to mice two times/day for a 28 day period. The 0.5% Tylose serves as a placebo. Six hours after the last treatment, the animals are sacrificed and livers are removed and immediately frozen for subsequent analysis. Blood is obtained by cardiac puncture of the anesthesized animals.
保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
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