GKT136901 hydrochloride T38646

Product Introduction
Bioactivity


英文名: GKT136901 hydrochloride

描述: GKT136901 hydrochloride is a powerful, selective, and orally active inhibitor of NADPH oxidase (NOX1/4). It exhibits K i values of 160 nM and 165 nM against NOX1 and NOX4, respectively. Additionally, GKT136901 hydrochloride demonstrates selectivity and direct scavenging ability towards peroxynitrite. This compound finds utility in studying diabetic nephropathy, stroke, neurodegeneration, and possesses anti-inflammatory properties.

体外活性: 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].

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: GKT-136901 Hydrochloride | GKT136901 Hydrochloride | GKT-136901 hydrochloride | GKT 136901 Hydrochloride

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