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GKT137831 

Cat. No.: HY-12298 Purity: 99.43%
Data Sheet SDS Handling Instructions

GKT137831 is a novel, specific dual NADPH oxidase (NOX1/4) inhibitor. GKT137831 has potency both on human Nox4 (Ki=140±40 nM) and human Nox1 (Ki=110±30 nM) and is found 15-fold less potent on Nox2 (Ki=1750±700 nM) and 3-fold less potent on Nox5 (Ki=410±100 nM).

For research use only. We do not sell to patients.
GKT137831 Chemical Structure

GKT137831 Chemical Structure

CAS No. : 1218942-37-0

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10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $140 In-stock
50 mg $450 In-stock
100 mg $640 In-stock
200 mg $950 In-stock
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    GKT137831 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2016 Dec 6;86:32-40.

    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.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GKT137831 is a novel, specific dual NADPH oxidase (NOX1/4) inhibitor. GKT137831 has potency both on human Nox4 (Ki=140±40 nM) and human Nox1 (Ki=110±30 nM) and is found 15-fold less potent on Nox2 (Ki=1750±700 nM) and 3-fold less potent on Nox5 (Ki=410±100 nM).

    IC50 & Target

    Ki: 140±40 nM (Nox4), 110±30 nM (Nox1)[1]

    In Vitro

    GKT137831 is a potent Nox4 inhibitor (Ki=120±30 nM) with an affinity similar to the irreversible and unspecific flavoprotein inhibitor Diphenyliodonium (DPI; Ki=70±10 nM)[1]. Administration of 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, 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 GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation[2].

    In Vivo

    During the last half of CCl4 injections, some mice are treated with 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 GKT137831 treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with GKT137831, to a level similar to that of WT mice given the NOX1/4 inhibitor[1].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2533 mL 1.2663 mL 2.5326 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    GKT137831 is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 1%) before use[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. 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]

    GKT137831 is prepared in corn oil[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 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 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
    Molecular Weight

    394.85

    Formula

    C₂₁H₁₉ClN₄O₂

    CAS No.

    1218942-37-0

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 37 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.43%

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    GKT137831
    Cat. No.:
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