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GKT136901

CAT: 0804-HY-101499-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-101499-01Size:5 mg
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Description
GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity[1][2][3].
CAS Number
955272-06-7
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
NADPH Oxidase
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Metabolic Disease; Inflammation/Immunology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/gkt136901.html
Purity
99.70
Solubility
DMSO : 33.33 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O
Molecular Formula
C19H15ClN4O2
Molecular Weight
366.80
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NOX1; NOX4

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