1. Metabolic Enzyme/Protease
  2. NADPH Oxidase
  3. GKT136901

GKT136901 

Cat. No.: HY-101499
Handling Instructions

GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 also is 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.

For research use only. We do not sell to patients.

GKT136901 Chemical Structure

GKT136901 Chemical Structure

CAS No. : 955272-06-7

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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 also is 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].

IC50 & Target

Ki: 160 (NOX1), 165 (NOX4)[1]

In Vitro

GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O2•− production and in H2O2 generation in MPT cells[4].
GKT136901 (10 μM; 30 min) abolishes the effect of high D-glucose on p38MAP kinase activation in MPT cells[4].
GKT136901 (10 μM; 2 h) attenuates methamphetamine (METH)-induced oxidative stress in HBMECs[5].
GKT136901 (10 μM; 2 h) protects HBMECs against METH-induced blood-brain barrier (BBB) dysfunction[5].

In Vivo

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes[6].

Animal Model: Male db/db and db/m mice (8 weeks)[6]
Dosage: 30, 90 mg/kg
Administration: Daily p.o. for 16 weeks
Result: Reduced albuminuria, thiobarbituric acid-reacting substances (TBARS) and renal ERK1/2 phosphorylation and preserved renal structure in diabetic mice.
Had no effect on plasma glucose, BP (blood pressure), and body weight.
Molecular Weight

366.80

Formula

C₁₉H₁₅ClN₄O₂

CAS No.

955272-06-7

SMILES

O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GKT136901GKT 136901GKT-136901NADPH OxidaseNOXNADPHoxidaseNOX1/4scavengerperoxynitritediabeticnephropathystrokeneurodegenerationanti-inflammatoryInhibitorinhibitorinhibit

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