GKT136901|cas:955272-06-7|西域试剂

GKT136901,99.12%

产品编号：Bellancom-101499| CAS NO：955272-06-7| 分子式：C₁₉H₁₅ClN₄O₂| 分子量：366.80

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货号	价格	库存与货期
Bellancom-101499	￥500.00	杭州北京（现货）
Bellancom-101499	￥750.00	杭州北京（现货）
Bellancom-101499	￥1400.00	杭州北京（现货）
Bellancom-101499	￥2000.00	杭州北京（现货）
Bellancom-101499	￥2800.00	杭州北京（现货）

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GKT136901

产品介绍

GKT136901 是一种有效的，选择性的和具有口服活性的 NADPH 氧化酶 NOX-1/4 抑制剂，K_i 值分别为 160 和 165 nM。GKT136901 也是一种选择性和直接的过氧亚硝酸清除剂。GKT136901 可用于糖尿病肾病，中风和神经退行性疾病的研究。GKT136901 还具有抗炎症活性。

生物活性

GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with K_is 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.

体外研究

GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O₂^•− production and in H₂O₂ 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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes^[6].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes^[6].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (90.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7263 mL	13.6314 mL	27.2628 mL
5 mM	0.5453 mL	2.7263 mL	5.4526 mL
10 mM	0.2726 mL	1.3631 mL	2.7263 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式