2. Anti-infection
  3. HBV
  4. Bay 41-4109

BAY 41-4109是人乙型肝炎病毒 (HBV) 的有效抑制剂，IC50值为 53 nM。

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Bay 41-4109 Chemical Structure

Bay 41-4109 Chemical Structure

CAS No. : 298708-81-3

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Other Forms of Bay 41-4109:

Bay 41-4109 相关抗体

Top Publications Citing Use of Products

    Bay 41-4109 purchased from MCE. Usage Cited in: Antiviral Res. 2018 Nov;159:1-12.  [Abstract]

    HepG2 cells are transfected with the indicated core protein-expressing plasmid. Six hours post transfection, the cells are left untreated or treated with 5 µM of BA38017, 5 µM of ENAN-34017 or 2 µM of Bay 41-4109 for 72 h. The cytoplasmic capsids are analyzed by a particle gel assay.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.

    IC50 & Target

    IC50&Target: 53 nM (HBV)[1]
    体外研究
    (In Vitro)

    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[2]. 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[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Bay 41-4109 相关抗体:
    体内研究
    (In Vivo)

    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[1].BAY41-4109 inhibits virus production in vivo by a mechanism that targets the viral capsid[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    395.76

    Formula

    C18H13ClF3N3O2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (252.68 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5268 mL 12.6339 mL 25.2678 mL
    5 mM 0.5054 mL 2.5268 mL 5.0536 mL
    查看完整储备液配制表

    * 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。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料
    参考文献
    Cell Assay
    [3]

    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, 20 μL of MTT solution (5 g/L) are added to each well and incubated at 37°C for 4 h. Next, 150 μL of DMSO is added and stirred for 10 min to dissolve the crystals. Absorbance values are recorded at 490 nm by using an ELISA reader. The MTT values are calculated using the curve regression equation[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Bay 41-4109 相关分类

    完整储备液配制表

    * 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。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5268 mL 12.6339 mL 25.2678 mL 63.1696 mL
    5 mM 0.5054 mL 2.5268 mL 5.0536 mL 12.6339 mL
    10 mM 0.2527 mL 1.2634 mL 2.5268 mL 6.3170 mL
    15 mM 0.1685 mL 0.8423 mL 1.6845 mL 4.2113 mL
    20 mM 0.1263 mL 0.6317 mL 1.2634 mL 3.1585 mL
    25 mM 0.1011 mL 0.5054 mL 1.0107 mL 2.5268 mL
    30 mM 0.0842 mL 0.4211 mL 0.8423 mL 2.1057 mL
    40 mM 0.0632 mL 0.3158 mL 0.6317 mL 1.5792 mL
    50 mM 0.0505 mL 0.2527 mL 0.5054 mL 1.2634 mL
    60 mM 0.0421 mL 0.2106 mL 0.4211 mL 1.0528 mL
    80 mM 0.0316 mL 0.1579 mL 0.3158 mL 0.7896 mL
    100 mM 0.0253 mL 0.1263 mL 0.2527 mL 0.6317 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Bay 41-4109298708-81-3HBVHepatitis B virusInhibitorinhibitorinhibit

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    目录号：
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