Setanaxib (GKT137831)

Catalog No.S7171 Synonyms: GKT831

For research use only.

Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.

Setanaxib (GKT137831) Chemical Structure

CAS No. 1218942-37-0

Selleck's Setanaxib (GKT137831) has been cited by 47 publications

Purity & Quality Control

Choose Selective NADPH-oxidase Inhibitors

Biological Activity

Description Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.
Targets
Ferroptosis [5] NOX1 [1]
(Cell-based assay)
NOX4 [1]
(Cell-based assay)
110 nM(Ki) 140 nM(Ki)
In vitro

GKT137831 attenuates hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs. [2] GKT137831 also prevents oxidative stress in response to hyperglycemia in human aortic endothelial cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HPAECs MVHQdo9tcW[ncnH0bY9vKGG|c3H5 MVWwMlEuOjBizszN M{f1dlI1KGh? NYSz[XRSdm9ic3nncolncWOjboSg[YZn\WO2IH;uJJBzd2yrZnXyZZRqd25? NGfwWVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmwOFE6QCd-MkK5NFQyQTh:L3G+
HPASMCs MXjQdo9tcW[ncnH0bY9vKGG|c3H5 NVqze|JtOC5zLUKwJO69VQ>? NXfCb|V2OjRiaB?= NEnFZZlifHSnboXheIVlKGOnbHygdJJwdGmoZYLheIlwdg>? NXLMfplnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5NFQyQThpPkKyPVA1OTl6PD;hQi=>
In vivo

In WT and SOD1mut mice, GKT137831 (60 mg/kg i.g.) blocks liver fibrosis and downregulates markers of oxidative stress, inflammation, and fibrosis. [1] GKT137831 (60 mg/kg/d p.o.) also attenuates chronic hypoxia–induced right ventricular hypertrophy, vascular remodeling, lung cell proliferation, and hypoxic alterations in lung PPARγ and TGF-β1 expression in mouse model of chronic hypoxia exposure. [2] In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. [3] Moreover, in angII-infused c-hNox4Tg mice, GKT137831 abolishes the increase in oxidative stress, suppresses Akt-mTOR and NF-κB signaling pathway and attenuates cardiac remodeling. [4]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Hypoxic HPASMC and HPAECs
  • Concentrations: 20 μM
  • Incubation Time: 72 hours
  • Method:

    Hypoxic HPASMC and HPAEC proliferation is determined using MTT assay, by Western blotting to detect proliferating cell nuclear antigen (PCNA) expression, or by manual cell counting after Trypan blue staining. Amplex Red Hydrogen Peroxide/Peroxidase Assay Kit is used to measure H2O2 released into the culture media from HPAECs or HPASMCs. After exposure to control or hypoxic environments for 72 hours, Amplex Red reagent is added, and the cells are returned to control or hypoxic environments for an additional hour before fluorescence measurements.

Animal Research:

[1]

  • Animal Models: Mouse models of liver fibrosis
  • Dosages: 60 mg/kg daily
  • Administration: i.g.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+2% Tween 80+30% PEG 300+ddH2O
For best results, use promptly after mixing.

9mg/mL

Chemical Information

Molecular Weight 394.85
Formula

C21H19ClN4O2

CAS No. 1218942-37-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C(=O)C=C2C(=C1C3=CC(=CC=C3)N(C)C)C(=O)N(N2)C4=CC=CC=C4Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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