GKT136901 hydrochloride

Research use only, not for human use.

GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.

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.

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Animal Model:Male db/db and db/m mice (8 weeks)Dosage:30, 90 mg/kg Administration:Daily p.o. for 16 weeksResult: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.

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Membrane Transporter/Ion Channel

NADPH

NADPH-oxidase

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1254507-01-1

403.26

C19H16Cl2N4O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (154.99 mM; Ultrasonic ) H2O : 4 mg/mL (9.92 mM; Ultrasonic (<60°C))

Cl.O=C1C=C2NN(C(=O)C2=C(N1CC3=NC=CC=C3)C)C=4C=CC=CC4Cl

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(-20℃)

With Ice Pack

≥ 2 years