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

Setanaxib  (Synonyms: GKT137831; GKT831)

Cat. No.: HY-12298 Purity: 99.45%
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Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.

For research use only. We do not sell to patients.

Setanaxib Chemical Structure

Setanaxib Chemical Structure

CAS No. : 1218942-37-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
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10 mg USD 120 In-stock
50 mg USD 408 In-stock
100 mg USD 650 In-stock
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Customer Review

Based on 27 publication(s) in Google Scholar

Setanaxib Related Antibodies

Top Publications Citing Use of Products

    Setanaxib purchased from MedChemExpress. 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 MedChemExpress. 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.

    View All NADPH Oxidase Isoform Specific Products:

    View All Isoforms
    NOX1 NOX2 NOX4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    NOX1

     

    NOX4

     

    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].

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

    Setanaxib Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    394.85

    Formula

    C21H19ClN4O2
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C3=CC=CC(N(C)C)=C3)N4C)=CC4=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (316.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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    Concentration
    ×
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.33 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.45%

    SDS (393 KB)

    COA (258 KB) HNMR (276 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References
    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.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 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
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    Setanaxib Related Classifications

    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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