GKT136901

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Chemical Structure| 955272-06-7 同义名 : NOX Inhibitor IV
CAS号 : 955272-06-7
货号 : A110729
分子式 : C19H15ClN4O2
纯度 : 99%+
分子量 : 366.801
MDL号 : MFCD09961532
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(95.42 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.63mL

2.73mL

1.36mL

27.26mL

5.45mL

2.73mL

参考文献

[1]Laleu B, et, al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem. 2010 Nov 11;53(21):7715-30.

[2]Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669.

[3]Schildknecht S, et, al. The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr Med Chem. 2014;21(3):365-76.

[4]Sedeek M, et, al. Critical role of Nox4-based NADPH oxidase in glucose-induced oxidative stress in the kidney: implications in type 2 diabetic nephropathy. Am J Physiol Renal Physiol. 2010 Dec;299(6):F1348-58.

[5]Hwang JS, et, al. GKT136901 protects primary human brain microvascular endothelial cells against methamphetamine-induced blood-brain barrier dysfunction. Life Sci. 2020 Sep 1;256:117917.

[6]Sedeek M, et, al. Renoprotective effects of a novel Nox1/4 inhibitor in a mouse model of Type 2 diabetes. Clin Sci (Lond). 2013 Feb;124(3):191-202.