Setanaxib (GKT137831)

For research use only.

Catalog No.S7171

23 publications

Setanaxib (GKT137831) Chemical Structure

Molecular Weight(MW): 394.85

GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectivelyl; ~10-fold selectivity towards NOX1, 4 and 5 over NOX2, does not inhibit XO or scavange ROS/RNS.

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Selleck's Setanaxib (GKT137831) has been cited by 23 publications

Purity & Quality Control

Choose Selective NADPH-oxidase Inhibitors

Biological Activity

Description GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectivelyl; ~10-fold selectivity towards NOX1, 4 and 5 over NOX2, does not inhibit XO or scavange ROS/RNS.
Targets
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 NYX1RY1[WHKxbHnm[ZJifGmxbjDhd5NigQ>? NV3hOIhGOC5zLUKwJO69VQ>? NIjHUYozPCCq NGfjZoVvdyC|aXfubYZq[2GwdDDl[oZm[3Rib36gdJJwdGmoZYLheIlwdg>? NInlOXEzOjlyNEG5PC=>
HPASMCs NHv2blRRem:uaX\ldoF1cW:wIHHzd4F6 NVnlbWQ4OC5zLUKwJO69VQ>? NIfRVoozPCCq NFXLOmdifHSnboXheIVlKGOnbHygdJJwdGmoZYLheIlwdg>? MYeyNlkxPDF7OB?=

... Click to View More Cell Line Experimental Data

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

Cell Research:

[2]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Mouse models of liver fibrosis
  • Dosages: 60 mg/kg daily
  • Administration: i.g.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL warmed (197.54 mM)
Water Insoluble
Ethanol Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 394.85
Formula

C21H19ClN4O2

CAS No. 1218942-37-0
Storage powder
in solvent
Synonyms N/A
Smiles CN(C)C1=CC=CC(=C1)C2=C3C(=O)N(NC3=CC(=O)N2C)C4=CC=CC=C4Cl

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID