CAS:1208315-24-5N6022

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N6022 reversibly inhibits s-nitrosoglutathione reductase (GSNOR) with IC50 and Ki of 8 nM, 2.5 nM, respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1208315-24-5

储存条件

分子式

C24H22N4O3

运输

蓝冰

分子量

414.46

别名

溶解度

DMSO	46.0 mg/mL (111.0 mM)
Water	Insoluble

动物实验配方

生物活性

描述S-Nitrosoglutathione reductase (GSNOR) is a zinc-dependent, NAD⁺- and NADH-dependent, medium chain alcohol dehydrogenase (ADH) that plays an important role in nitrosative biology by metabolizing the S-nitrosothiol, GSNO. N6022 is a potent, selective and reversible GSNOR inhibitor with an IC₅₀ of 8 nM and a K_i of 2.5 nM^[3]. In cytochrome P450 assays, N6022 potently inhibited CYP2C19 with an IC₅₀ of 0.77 μM. And it exhibited minimal cytotoxicity (IC₅₀ > 100 μM) toward A549 epithelial lung cells. In a mouse model of ovalbumin-induced asthma, N6022 attenuated methacholine-induced broncho-constriction (airway hyperresponsiveness) in a dose- and time-dependent manner, with significant efficacy achieved with a single IV dose ≥0.01 mg/kg^[4].
作用机制N6022 binds in the GSNO substrate binding pocket like a competitive inhibitor^[3].