GKT136901

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GKT136901

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

955272-06-7

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

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 ofNADPH oxidase(NOX1/4), withK_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^[1]^[2]^[3].

IC₅₀& Target

Ki: 160 (NOX1), 165 (NOX4)^[1]

体外研究
(In Vitro)

GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O₂^o–production and in H₂O₂generation 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].

体内研究
(In Vivo)

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:	Maledb/dbanddb/mmice (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.

分子量

366.80

性状

Solid

Formula

C₁₉H₁₅ClN₄O₂

CAS 号

955272-06-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。