2. Metabolic Enzyme/Protease Apoptosis
  3. NADPH Oxidase Ferroptosis
  4. Setanaxib

Setanaxib  (Synonyms: GKT137831; GKT831)

目录号: HY-12298 纯度: 99.45%
COA 产品使用指南

摩尔计算器

Setanaxib (GKT137831) 是选择性的NADPH氧化酶 (NOX1/4) 抑制剂，Ki 分别为140和110nM。

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Setanaxib Chemical Structure

Setanaxib Chemical Structure

CAS No. : 1218942-37-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥956
In-stock
2 mg ￥730
In-stock
5 mg ￥1100
In-stock
10 mg ￥1850
In-stock
50 mg ￥5275
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Setanaxib 相关抗体

Top Publications Citing Use of Products

    Setanaxib purchased from MCE. Usage Cited in: Antioxid Redox Signal. 2019 May 20;30(15):1831-1848.  [Abstract]

    The western blot assay shows that Tan-IIA and GKT137831 inhibit Smad3 activation in response to TGF-β1 by dephosphorylation.

    Setanaxib purchased from MCE. Usage Cited in: Biomed Pharmacother. 2016 Dec 6;86:32-40.  [Abstract]

    Effect of Rutin on TXNIP, NLRP3 and caspase-1 proteins expression. HUVECs or Nox4-overexpressed HUVECs are incubated indicated rutinor GKT for 48 h under indicated glucose condition. Bands of western blotting are analyzed by densitometry.

    查看 NADPH Oxidase 亚型特异性产品:

    查看所有亚型
    NOX1 NOX2 NOX4

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.

    IC50 & Target

    NOX1

     

    NOX4

     

    体外研究
    (In Vitro)

    Setanaxib (GKT137831) is a potent Nox1/4 inhibitor (Kis=140±40/110±30 nM)[1]. Administration of Setanaxib (GKT137831) throughout the 72-hour period of normoxia or hypoxia exposure attenuates HPASMC proliferation under normoxic conditions at the 20 μM concentration but had no effect on proliferation in normoxic HPAECs. In the prevention paradigm, Setanaxib (GKT137831) attenuates hypoxia-induced HPASMC and HPAEC proliferation at 5 and 20 μM. Complementary assays of cell proliferation measuring the expression of PCNA or manual cell counting confirmed that Setanaxib (GKT137831) attenuates hypoxia-induced pulmonary vascular cell proliferation[2].

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

    Setanaxib 相关抗体:
    体内研究
    (In Vivo)

    During the last half of CCl4 injections, some mice are treated with Setanaxib (GKT137831) daily. CCl4-induced liver fibrosis is more pronounced in SOD1mu compared to WT mice. Liver fibrosis in both SOD1mu and WT mice is attenuated by Setanaxib (GKT137831) treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with Setanaxib (GKT137831), to a level similar to that of WT mice given the NOX1/4 inhibitor[1].

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

    394.85

    Formula

    C21H19ClN4O2
    CAS 号
    性状

    固体

    颜色

    White 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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 125 mg/mL (316.58 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 2.5326 mL 12.6630 mL 25.3261 mL
    5 mM 0.5065 mL 2.5326 mL 5.0652 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (6.33 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.33 mM); 悬浊液; 超声助溶

    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

    纯度: 99.45%

    COA (202 KB) HNMR (276 KB) LCMS (96 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Monolayers of HPAECs and HPASMCs are propagated in culture and placed in normoxic (21% O2, 5% CO2) or hypoxic (1% O2, 5% CO2) conditions for 72 hours. Setanaxib (GKT137831) (0.1-20 μM), or vehicle (1% DMSO) are added to the culture medium at the onset (prevention regimen) or during the last 24 hours (intervention regimen) of a 72-hour hypoxia exposure regimen[2].

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

    Mice[1]
    Specific pathogen-free, wild-type (WT) C57BL/6J mice are used. For the carbon tetrachloride (CCl4) model of liver fibrosis, 6 week old male mice are injected intraperitoneally with CCl4, which is diluted 1:3 in corn oil, or with vehicle (corn oil) at a dose of 0.5 μL/g of body weight twice a week for a total of 12 injections. During the last half of CCl4 treatment, mice are treated with 60 mg/kg of the NOX1/4 inhibitor Setanaxib (GKT137831) or vehicle by intragastric injection daily. Mice are sacrificed 48 hours after the last CCl4 injection. For the bile duct ligation (BDL) model, 6 week old male mice are anesthetized. After laparotomy, the common bile duct is ligated twice and the abdomen closed. The sham operation is performed similarly without BDL. From 11 days after operation, mice are treated with 60 mg/kg of the NOX1/4 inhibitor Setanaxib (GKT137831) or vehicle by daily intragastric lavage. Mice are sacrificed 21 days after operation. Serum levels of alanine aminotransferase (ALT) are measured with a commercial kit.

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

    Setanaxib 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5326 mL 12.6630 mL 25.3261 mL 63.3152 mL
    5 mM 0.5065 mL 2.5326 mL 5.0652 mL 12.6630 mL
    10 mM 0.2533 mL 1.2663 mL 2.5326 mL 6.3315 mL
    15 mM 0.1688 mL 0.8442 mL 1.6884 mL 4.2210 mL
    20 mM 0.1266 mL 0.6332 mL 1.2663 mL 3.1658 mL
    25 mM 0.1013 mL 0.5065 mL 1.0130 mL 2.5326 mL
    30 mM 0.0844 mL 0.4221 mL 0.8442 mL 2.1105 mL
    40 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5829 mL
    50 mM 0.0507 mL 0.2533 mL 0.5065 mL 1.2663 mL
    60 mM 0.0422 mL 0.2111 mL 0.4221 mL 1.0553 mL
    80 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
    100 mM 0.0253 mL 0.1266 mL 0.2533 mL 0.6332 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:

    Setanaxib1218942-37-0GKT137831 GKT831GKT 137831GKT-137831GKT831GKT 831GKT-831NADPH OxidaseFerroptosisNOXInhibitorinhibitorinhibit

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