1. Metabolic Enzyme/Protease
  2. NADPH Oxidase
  3. ML171

ML171  (Synonyms: 2-乙酰基吩噻嗪; 2-Acetylphenothiazine; 2-APT)

目录号: HY-12805 纯度: 99.82%
COA 产品使用指南

ML171 (2-Acetylphenothiazine;2-APT) 是有效的选择性 NADPH 氧化酶 1 (Nox1) 抑制剂,可阻止 Nox-1 依赖性的 ROS 产生,在 HEK293-Nox1 验证试验中的 IC50 值为 0.25 μM。

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ML171 Chemical Structure

ML171 Chemical Structure

CAS No. : 6631-94-3

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥220
In-stock
100 mg ¥200
In-stock
500 mg ¥400
In-stock
1 g   询价  
5 g   询价  

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Top Publications Citing Use of Products

    ML171 purchased from MCE. Usage Cited in: Inflammation. 2023 Feb 20.  [Abstract]

    In rat NP cells, ML171 inhibits the expression of catabolic markers MMP13, ADAMTS4, ADAMTS5, and pyroptotic markers NLRP3, GSDMD-NT, and cleaved-caspase-1, as well as incresaes the expression of ECM anabolic markers COL2A and ACAN, by inhibiting overexpression of BRD9 (Fig. c and d).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.

    IC50 & Target

    NOX1

     

    体外研究
    (In Vitro)

    Nox1-dependent ROS generation has been shown to play a pivotal role in cell signaling, cell growth, angiogenesis, motility and blood pressure regulation. ML171 strongly blocks ROS generation in HT29 cells (IC50=0.129 μM) and only increasing over-expression of Nox1 can overcome the blockage of ROS generation caused by ML171 treatment in HEK293 cell system reconstituted with all the components required Nox1-dependent ROS generation. ML171 efficiently blocks ROS production measured by carboxy-H2-DCFDA staining as well as DPI used as a positive control. When ML171 is tested in HEK293-Nox1 reconstituted cell system, higher potency in blocking Nox1-dependent ROS generation is observed compared with the parental compound[1].

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

    分子量

    241.31

    Formula

    C14H11NOS

    CAS 号
    性状

    固体

    颜色

    Yellow to orange

    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 : ≥ 64 mg/mL (265.22 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 4.1440 mL 20.7202 mL 41.4405 mL
    5 mM 0.8288 mL 4.1440 mL 8.2881 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: ≥ 2.5 mg/mL (10.36 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。

      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。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (10.36 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,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 25.0 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

    纯度: 99.82%

    参考文献
    Cell Assay
    [1]

    HT29 cells are cultured in 150 mm diameter plate and when 70-80% confluence is reached, cells are trypsinized, harvested in HBSS and counted. 4×104 cells are dispensed into individual wells in 30 μL final volume (384 well plates) by using a robotic liquid handler. Cells are treated for 60 min at 37°C with 50 nL of DPI, DMSO and library compounds (including ML171) which are automatically dispensed into individual wells from their respective assay plates. This will correspond to a final concentration of 10 μM DPI or library compounds (ML171), and 0.1% DMSO. 20 μL of a mixture containing 200 μM luminol plus 0.32 units of HRP (final concentration) is added. Luminescence is quantified using a 384-well plate luminometer. The data output consisting of the emission intensities for each well is imported into a spread-sheet program (such as Excel) for further processing. As designed, compounds that inhibit Nox1 activity will reduce cellular ROS production, leading to reduced probe-ROS interactions and reduced well luminescence. Compounds are considered ‘hits’ and further processed when light emission is blocked >75% 7 than DMSO wells (DMSO and DPI wells are set to 0% and 100% respectively). Compounds are tested in singlicate at a concentration of 10 μM[1].

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

    参考文献

    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 4.1440 mL 20.7202 mL 41.4405 mL 103.6012 mL
    5 mM 0.8288 mL 4.1440 mL 8.2881 mL 20.7202 mL
    10 mM 0.4144 mL 2.0720 mL 4.1440 mL 10.3601 mL
    15 mM 0.2763 mL 1.3813 mL 2.7627 mL 6.9067 mL
    20 mM 0.2072 mL 1.0360 mL 2.0720 mL 5.1801 mL
    25 mM 0.1658 mL 0.8288 mL 1.6576 mL 4.1440 mL
    30 mM 0.1381 mL 0.6907 mL 1.3813 mL 3.4534 mL
    40 mM 0.1036 mL 0.5180 mL 1.0360 mL 2.5900 mL
    50 mM 0.0829 mL 0.4144 mL 0.8288 mL 2.0720 mL
    60 mM 0.0691 mL 0.3453 mL 0.6907 mL 1.7267 mL
    80 mM 0.0518 mL 0.2590 mL 0.5180 mL 1.2950 mL
    100 mM 0.0414 mL 0.2072 mL 0.4144 mL 1.0360 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:
    ML171
    目录号:
    HY-12805
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