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N6022

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Chemical Structure| 1208315-24-5 同义名 : -
CAS号 : 1208315-24-5
货号 : A502981
分子式 : C24H22N4O3
纯度 : 99%+
分子量 : 414.457
MDL号 : MFCD22123247
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(60.32 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 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 Ki 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL
参考文献

[1]Green LS, Chun LE, et al. Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. Biochemistry. 2012 Mar 13;51(10):2157-68.

[2]Sun X, Wasley JW, et al. Discovery of s-nitrosoglutathione reductase inhibitors: potential agents for the treatment of asthma and other inflammatory diseases. ACS Med Chem Lett. 2011 Mar 11;2(5):402-6.

[3]Green LS, Chun LE, et al. Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. Biochemistry. 2012 Mar 13;51(10):2157-68

[4]Sun X, Wasley JW, et al. Discovery of s-nitrosoglutathione reductase inhibitors: potential agents for the treatment of asthma and other inflammatory diseases. ACS Med Chem Lett. 2011 Mar 11;2(5):402-6