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Setanaxib

Catalog No. T6099 CAS 1218942-37-0

Synonyms: GKT137831

GKT137831 is a potent, specific dual NADPH oxidase (NOX1/4) inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Setanaxib, CAS 1218942-37-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GKT137831 is a potent, specific dual NADPH oxidase (NOX1/4) inhibitor.
Targets&IC50	NOX4:140 nM(Ki), NOX1:110 nM(Ki)
Kinase Assay	Kinase Assay: IC50 of tyrosine kinase activity is measured by an enzyme-linked immunosorbent assay (ELISA) with recombinant catalytic domains of a panel of receptor and non-receptor tyrosine kinases (in some cases only part of the catalytic domain is used). Saracatinib dose ranges from 0.001-10 mM. Speci?city assays against a panel of serine/threonine kinases are performed using a ?lter capture assay with 32P. Brie?y, multidrop 384 plates containing 0.5 μL Saracatinib or controls (DMSO) alone or pH 3.0 buffer controls) are incubated with 15 μL of enzyme plus peptide/protein substrate for 5 min before the reaction is initiated by the addition of 10 μL of 20 mM Mg-ATP. For all enzymes the ?nal concentration is approximated to the Michaelis constant (Km). Assays are carried out for 30min at room temperature before termination by the addition of 5 μL orthophosphoric acid. After mixing, the well contents are harvested onto a P81 Uni?lter plate, using orthophosphoric acid as the wash buffer. Then IC50 is calculated.
Cell Research	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 Water2 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)

Synonyms	GKT137831
Molecular Weight	394.85
Formula	C21H19ClN4O2
CAS No.	1218942-37-0

Storage

store at low temperture,keep away from direct sunlight

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 72 mg/mL (182.3 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Aoyama T, et al. Hepatology. 2012, 56(6), 2316-2327. 2. Green DE, et al. Am J Respir Cell Mol Biol. 2012, 47(5), 718-726. 3. Gray SP, et al. Circulation. 2013, 127(18), 1888-1902. 4. Zhao QD, et al. 2015, Doi:10.1161/CIRCULATIONAHA.114. 2011079.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

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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:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Reconstitution Calculation

Molecular Weight Calculator

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Mass of a compound required to prepare a solution of known volume and concentration
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An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
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The answer of 19.713 mg appears in the Mass box

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Calculator the dilution required to prepare a stock solution

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The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Molecule Formula

Molecular Weight g/mol

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Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Setanaxib 1218942-37-0 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation Metabolism NADPH-oxidase Ferroptosis NADPH NOX GKT-137831 GKT 137831 GKT-831 GKT831 inhibit GKT 831 Inhibitor GKT137831 NADPH Oxidase inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.