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.

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[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].

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.

1254507-01-1

C19H16Cl2N4O2

403.26

GKT136901 hydrochloride;GKT136901 hydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years