GKT136901 hydrochloride

GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4) , with K i s 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

In Vitro

GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O 2 •− production and in H 2 O 2 generation in MPT cells . GKT136901 (10 μM; 30 min) abolishes the effect of high D-glucose on p38MAP kinase activation in MPT cells . GKT136901 (10 μM; 2 h) attenuates methamphetamine (METH)-induced oxidative stress in HBMECs . GKT136901 (10 μM; 2 h) protects HBMECs against METH-induced blood-brain barrier (BBB) dysfunction . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male db/db and db/m mice (8 weeks) 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.

Form:Solid

IC50& Target:Ki: 160 (NOX1), 165 (NOX4)