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GSK2795039 NADPH-oxidase inhibitor

Name: GSK2795039
Brand: Selleck Chemicals
SKU: S8974
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8974

GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. This compound inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.

Chemical Structure

Molecular Weight: 450.56

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Quality Control

Batch: S897401 DMSO]125 mg/mL]true]Ethanol]20 mg/mL]false]Water]Insoluble]false Purity: 99.77%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.77

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other NADPH-oxidase Inhibitors	Setanaxib (GKT137831) NAD+ (β-DPN) DPI (Diphenyleneiodonium chloride) Apocynin GLX351322 2-Acetylphenothiazine (ML171) VAS2870 gp91ds-tat Isuzinaxib (APX-115 free base)

Solubility

In vitro
Batch:

DMSO : 125 mg/mL (277.43 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.	10.000mg/ml (22.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 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 make it clear; 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.

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.

Chemical Information, Storage & Stability

Molecular Weight	450.56	Formula	C₂₃H₂₆N₆O₂S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1415925-18-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)N1C=C(C2=C(C=CN=C21)NS(=O)(=O)C3=NN(C=C3)C)C4=CC5=C(CCN5C)C=C4

Mechanism of Action

Targets/IC₅₀/Ki	ROS NADPH NOX2 (HRP/Amplex Red) (Cell-based assay) 6.57(pIC50)
In vitro	GSK2795039 inhibits both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. This compound inhibits NOX2 in an NADPH competitive manner and is selective over other NOX isoforms, xanthine oxidase, and endothelial nitric oxide synthase enzymes.
In vivo	Following systemic administration in mice, GSK2795039 abolishes the production of ROS by activated NOX2 enzyme in a paw inflammation model. This compound shows activity in a murine model of acute pancreatitis, reducing the levels of serum amylase triggered by systemic injection of cerulein.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26135714/ [2] https://pubmed.ncbi.nlm.nih.gov/30777083/

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