1. Metabolic Enzyme/Protease
  2. Elastase
  3. BAY-85-8501

BAY-85-8501 是人类中性脂酶 (HNE) 的一个有效的、选择性抑制剂,其 IC50 值为 65 pM。

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BAY-85-8501 Chemical Structure

BAY-85-8501 Chemical Structure

CAS No. : 1161921-82-9

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10 mM * 1 mL in DMSO ¥4700
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1 mg ¥2200
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5 mg ¥4500
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10 mg ¥6700
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Top Publications Citing Use of Products
Proliferation Assay

    BAY-85-8501 purchased from MCE. Usage Cited in: Chinese Academy of Sciences. 2019 Aug.

    Blood from 3 healthy individuals, was separated using Lymhoprep, neutrophils isolated and plated out in 96 well plates at 5x105 and incubated with PMA (50 nM) for 3 hours, with and without inhibitor as above. Results show that BAY-85-8501 inhibits human neutrophil elastase at all 3 concentrations (50, 25, and 12.5 µM) with a significance of P<0.0001, when compared to the positive control of human neutrophil elastase and cells incubated with PMA and vehicle.
    • 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-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.

    IC50 & Target

    IC50: 65 pM (HNE)[1].

    体内研究
    (In Vivo)

    In this model the exogenous HNE noxa is the primary cause of injury and lung hemorrhage. Based on picomolar potency against HNE as well as single digit potency versus MNE, BAY-85-8501 (29) completely prevents the development of lung injury and subsequent inflammation when administered 1 h prior to the HNE noxa. In the 0.01 mg/kg dose group, hemoglobin concentration is already significantly decreased. At a dose of 0.1 mg/kg, a significant effect on neutrophil count is observed. In this setup, efficacy is predominantly driven by potency against HNE (Ki=0.08 nM). As the highly HNE-selective inhibitor BAY 85-8501 has no effect on PPE, BAY-85-8501 could not prevent the primary lung injury in this setup. Nevertheless, BAY-85-8501 could inhibit MNE, the endogenous driver of inflammation and secondary injury, although with decreased potency. Consequently, the effects of BAY-85-8501 on inflammation and secondary injury are weaker at this point, and only observed at 30-fold higher doses. Efficacy is predominantly driven by potency against MNE (Ki=6 nM) in this second setup[1].

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

    分子量

    474.46

    Formula

    C22H17F3N4O3S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    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
    In Vitro: 

    DMSO 中的溶解度 : 200 mg/mL (421.53 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 2.1077 mL 10.5383 mL 21.0766 mL
    5 mM 0.4215 mL 2.1077 mL 4.2153 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

    In Vivo:

    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: ≥ 5 mg/mL (10.54 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 50.0 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。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 5 mg/mL (10.54 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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

    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
    Animal Administration
    [1]

    Mice[1]
    Elastaseinduced lung failure in mice, rats or hamsters is a widely used animal model of acute lung failure. The animals are treated 1 hour prior to orotracheal instillation of human neutrophil elastase (HNE) or porcine pancreatic elastase (PPE). In this study, each mouse receives BAY-85-8501 with different concentrations (0.003, 0.01, 0.03, 0.1, 0.3, 3, 10, 30 mg/kg) by P.O.[1].

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

    参考文献

    BAY-85-8501 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 2.1077 mL 10.5383 mL 21.0766 mL 52.6915 mL
    5 mM 0.4215 mL 2.1077 mL 4.2153 mL 10.5383 mL
    10 mM 0.2108 mL 1.0538 mL 2.1077 mL 5.2691 mL
    15 mM 0.1405 mL 0.7026 mL 1.4051 mL 3.5128 mL
    20 mM 0.1054 mL 0.5269 mL 1.0538 mL 2.6346 mL
    25 mM 0.0843 mL 0.4215 mL 0.8431 mL 2.1077 mL
    30 mM 0.0703 mL 0.3513 mL 0.7026 mL 1.7564 mL
    40 mM 0.0527 mL 0.2635 mL 0.5269 mL 1.3173 mL
    50 mM 0.0422 mL 0.2108 mL 0.4215 mL 1.0538 mL
    60 mM 0.0351 mL 0.1756 mL 0.3513 mL 0.8782 mL
    80 mM 0.0263 mL 0.1317 mL 0.2635 mL 0.6586 mL
    100 mM 0.0211 mL 0.1054 mL 0.2108 mL 0.5269 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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    产品名称:
    BAY-85-8501
    目录号:
    HY-19908
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