产品
编 号：F743567
分子式：C19H16Cl2N4O2
分子量：403.26
分子式：C19H16Cl2N4O2
分子量：403.26
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
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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结构图
CAS No: 1254507-01-1
产品详情
生物活性：
GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis 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.
体内研究：
GKT136901 hydrochloride (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 hydrochloride (10 μM；30 分钟) 显著降低高 d -葡萄糖诱导的 MPT 细胞中 O2?-生成和 H2O2 生成的增加。 GKT136901 hydrochloride (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 hydrochloride (10 μM；2 小时) 减弱 HBMEC 中甲基苯丙胺 (METH) 诱导的氧化应激。 GKT136901 hydrochloride (10 μM；2 小时) 保护 HBMEC 免受 METH 诱导的血脑屏障 (BBB) 功能障碍。
GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis 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.
体内研究：
GKT136901 hydrochloride (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 hydrochloride (10 μM；30 分钟) 显著降低高 d -葡萄糖诱导的 MPT 细胞中 O2?-生成和 H2O2 生成的增加。 GKT136901 hydrochloride (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 hydrochloride (10 μM；2 小时) 减弱 HBMEC 中甲基苯丙胺 (METH) 诱导的氧化应激。 GKT136901 hydrochloride (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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