Comparison

GKT136901 (hydrochloride) European Partner

Item no. HY-101499A-10mM
Manufacturer MedChem Express
CASRN 1254507-01-1
Amount 10mM/1mL
Quantity options 100 mg 10mM/1mL 10 mg 25 mg 50 mg 5 mg
Category
Type Biochemicals
Specific against other
Purity 99.90
Formula C19H16Cl2N4O2
Citations [1]Hwang JS, et, al. GKT136901 protects primary human brain microvascular endothelial cells against methamphetamine-induced blood-brain barrier dysfunction. Life Sci. 2020 Sep 1;256:117917.<br>[2]Sedeek M, et, al. Renoprotective effects of a novel Nox1/4 inhibitor in a mouse model of Type 2 diabetes. Clin Sci (Lond). 2013 Feb;124(3):191-202.<br>[3]Laleu B, et, al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem. 2010 Nov 11;53(21):7715-30.<br>[4]Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669.<br>[5]Schildknecht S, et, al. The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr Med Chem. 2014;21(3):365-76.<br>[6]Sedeek M, et, al. Critical role of Nox4-based NADPH oxidase in glucose-induced oxidative stress in the kidney: implications in type 2 diabetic nephropathy. Am J Physiol Renal Physiol. 2010 Dec;299(6):F1348-58.
Smiles O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O.[H]Cl
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Available
Product Description
GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 hydrochloride is also a selective and direct scavenger of peroxynitrite. GKT136901 hydrochloride can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 hydrochloride also has anti-inflammatory activity[1][2][3].
StorageTemperature
4°C (Powder, sealed storage, away from moisture)
Shipping
Room Temperature
Manufacturers Applications
Metabolism-sugar/lipid metabolism
MolecularWeight
403.26
Clinical_Information
No Development Reported
Manufacturers Research Area
Metabolic Disease; Neurological Disease
Solubility
DMSO : 62.5 mg/mL (ultrasonic)|H2O : 4 mg/mL (ultrasonic; warming; heat to 60°C)
Manufacturers Target
NADPH Oxidase
Isoform
NOX1; NOX4
Pathway
Metabolic Enzyme/Protease

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 10mM/1mL
Available: In stock
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