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Setanaxib (GKT137831) NOX1/4 Inhibitor

Name: Setanaxib (GKT137831)
Brand: Selleck Chemicals
SKU: S7171
Rating: 5 (72 reviews)

Cat.No.S7171

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

Chemical Structure

Molecular Weight: 394.85

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other NADPH-oxidase Inhibitors	NAD+ (β-DPN) DPI (Diphenyleneiodonium chloride) Apocynin 2-Acetylphenothiazine (ML171) GLX351322 GSK2795039 VAS2870 gp91ds-tat Isuzinaxib (APX-115 free base)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
HPAECs	Proliferation assay	0.1-20 μM	24 h	no significant effect on proliferation	22904198
HPASMCs	Proliferation assay	0.1-20 μM	24 h	attenuated cell proliferation	22904198
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	394.85	Formula	C₂₁H₁₉ClN₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1218942-37-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GKT831			Smiles	CN1C(=O)C=C2C(=C1C3=CC(=CC=C3)N(C)C)C(=O)N(N2)C4=CC=CC=C4Cl

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (197.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (7.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	Ferroptosis NOX1 (Cell-based assay) 110 nM(Ki) NOX4 (Cell-based assay) 140 nM(Ki)
In vitro	Setanaxib (GKT137831) attenuates hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs. It also prevents oxidative stress in response to hyperglycaemia in human aortic endothelial cells.
In vivo	In WT and SOD1mut mice, Setanaxib (GKT137831) (60 mg/kg i.g.) blocks liver fibrosis and downregulates markers of oxidative stress, inflammation, and fibrosis. This compound (60 mg/kg/d p.o.) also attenuates chronic hypoxia–induced right ventricular hypertrophy, vascular remodelling, lung cell proliferation, and hypoxic alterations in lung PPARγ and TGF-β1 expression in mouse model of chronic hypoxia exposure. In diabetic apolipoprotein E-deficient mice, it (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. Moreover, in angII-infused c-hNox4Tg mice, it abolishes the increase in oxidative stress, suppresses Akt-mTOR and NF-κB signalling pathway and attenuates cardiac remodelling.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22806357/ [2] https://pubmed.ncbi.nlm.nih.gov/22904198/ [3] https://pubmed.ncbi.nlm.nih.gov/23564668/ [4] https://pubmed.ncbi.nlm.nih.gov/25589557/ [5] https://pubmed.ncbi.nlm.nih.gov/31173656/

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Handling Instructions

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