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

BAY 41-4109是人乙型肝炎病毒 (HBV) 的有效抑制劑，IC50值為 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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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1430
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5 mg ￥1300
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10 mg ￥2200
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50 mg 現(xiàn)貨 詢價
100 mg   詢價  
200 mg   詢價  

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Customer Review

Other Forms of Bay 41-4109:

    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

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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]
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HepG2 2.2.15 CC50
    > 5 μM
    Compound: Bay41-4109; 1
    Cytotoxicity in human HepG2.2.15 cells assessed as reduction in cell viability incubated for 8 days by MTT assay
    Cytotoxicity in human HepG2.2.15 cells assessed as reduction in cell viability incubated for 8 days by MTT assay
    		[PMID: 32692159]
    HepG2 2.2.15 IC50
    0.042 μM
    Compound: Bay41-4109; 1
    Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic HBV-DNA replication incubated for 8 days by real-time PCR analysis
    Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic HBV-DNA replication incubated for 8 days by real-time PCR analysis
    		[PMID: 32692159]
    HepG2 2.2.15 CC50
    19.3 μM
    Compound: 4; Bay41-4109
    Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
    Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
    		[PMID: 28082068]
    體外研究
    (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.
    體內(nèi)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 號
    性狀

    固體

    顏色

    Light yellow to yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 100 mg/mL (252.68 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料
    參考文獻
    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.
    參考文獻

    Bay 41-4109 相關分類

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    產(chǎn)品名稱：
    Bay 41-4109
    目錄號：
    HY-100029
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