Setanaxib (GKT137831)

This product is for research use only, not for human use. We do not sell to patients.

Setanaxib (GKT137831)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$445In Stock
250mg$800In Stock
500mg$1200In Stock

Cat #: V1904 CAS #: 1218942-37-0 Purity ≥ 98%

Description: Setanaxib (also known as GKT-137831; GTK831) is a novel, specific, potent, orally bioavailable, and dual inhibitor of NADPH oxidase NOX1/NOX4 with Ki of 110 nM and 140 nM, respectively.

References: Aoyama T, et al. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology. 2012 Dec;56(6):2316-27.

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Molecular Weight (MW)394.85
Molecular FormulaC21H19ClN4O2
CAS No.1218942-37-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 78 mg/mL (197.5 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
SMILES CodeCN(C)C1=CC(C2=C(C(N(C3=CC=CC=C3Cl)N4)=O)C4=CC(N2C)=O)=CC=C1
SynonymsGTK831; GTK-831; GKT-137831; GKT137831; GKT 137831; GTK 831
ProtocolIn VitroSetanaxib (GKT137831) is a potent Nox1/4 inhibitor (Kis=140±40/110±30 nM).
In VivoDuring 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5326 mL12.6630 mL25.3261 mL50.6521 mL
5mM0.5065 mL2.5326 mL5.0652 mL10.1304 mL
10mM0.2533 mL1.2663 mL2.5326 mL5.0652 mL
20mM0.1266 mL0.6332 mL1.2663 mL2.5326 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.