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编 号:F538154
分子式:C19H15ClN4O2
分子量:366.8
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.

体内研究:
GKT136901 (30-90 mg/kg;每日口服,持续 16 周) 对 2 型糖尿病小鼠模型具有肾脏保护作用。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.

体外研究:
GKT136901 (10 μM;30 分钟) 显著减弱高MPT细胞中 D-葡萄糖诱导的 O2?? 产生和 H2O 2 的增加。 GKT136901 (10 μM;30 分钟) 消除高 D-葡萄糖对 MPT 细胞中 p38MAP 激酶激活的影响。 GKT136901 (10 μM;2 小时) 减弱 HBMEC 中甲基苯丙胺 (METH) 诱导的氧化应激。 GKT136901 (10 μM;2 小时) 保护 HBMEC 免受 METH 诱导的血脑屏障 (BBB) 功能障碍。
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