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GKT136901 (hydrochloride)
$50 – $280
Products Details
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].
Web ID
– HY-101499A
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Metabolism-sugar/lipid metabolism
Molecular Formula
– C19H16Cl2N4O2
References
– [1]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.|[2]Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669.|[3]Schildknecht S, et, al. The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr Med Chem. 2014;21(3):365-76.|[4]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.|[5]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.|[6]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.
CAS Number
– 1254507-01-1
Molecular Weight
– 403.26
Compound Purity
– 99.06
SMILES
– O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O.[H]Cl
Clinical Information
– No Development Reported
Research Area
– Metabolic Disease; Neurological Disease
Solubility
– DMSO : 62.5 mg/mL (ultrasonic)|H2O : 4 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– NADPH Oxidase
Isoform
– NOX1;NOX4
Pathway
– Metabolic Enzyme/Protease
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
