GKT136901 is a potent, selective and orally active inhibitor of NOX1/4, with Ki values of 160 and 165 nM, respectively. It also acts as a selective direct scavenger of peroxynitrite. GKT136901 is applicable in research for diabetic nephropathy, stroke, and neurodegenerative diseases. Additionally, it possesses anti-inflammatory properties[1][2][3]. Treating cells with GKT136901 at a concentration of 10 μM for 30 minutes significantly attenuates the increase in O2- production and H2O2 generation induced by high D-glucose in MPT cells. It also eliminates the effect of high D-glucose on the activation of p38MAP kinase in MPT cells[4]. A 2-hour treatment of cells with GKT136901 at a concentration of 10 μM can alleviate METH-induced oxidative stress in HBMEC and protect against METH-induced blood-brain barrier dysfunction in HBMEC[5].
GKT136901 动物研究
Animal study
Administered orally at a dosage of 30-90 mg/kg daily for 16 weeks, GKT136901 provides renal protection in a type 2 diabetes mouse model[6].
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