N6022

製品コードS7589 バッチS758901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H22N4O3
分子量 414.46 CAS No. 1208315-24-5
Solubility (25°C)* 体外 DMSO 82 mg/mL (197.84 mM)
Ethanol 5 mg/mL warmed with 50ºC water bath (12.06 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 N6022 is a selective, and reversible inhibitor of S-nitrosoglutathione reductase (GSNOR) with IC50 of 8 nM and Ki of 2.5 nM. Phase 1/2.
in vitro N6022 shows limited off-target activity and low cytotoxicity toward A549 epithelial lung cells. [2]
in vivo N6022 (30 mg/kg iv or po) reduces bronchoconstriction and pulmonary inflammation in a mouse model of asthma. [2]

プロトコル(参考用のみ)

キナーゼアッセイ GSNOR Assays
GSNOR activity for the reduction of GSNO is determined by measuring the NADH- and GSNO-dependent decrease in absorbance at 340 nm (A340). Progress curves are depicted as a decrease in absorbance over time due to NADH and GSNO consumption with a linear slope equal to the reaction velocity. Kinetic constants are determined at room temperature in 100 mM sodium phosphate buffer (pH 7.4) with a GSNOR concentration of 11 nM. For GSNO constants, NADH is at a fixed concentration of 300 μM while the GSNO concentration ranges from 0.5 to 240 μM. For the NADH constants, the GSNO concentration is fixed at 300 μM and the NADH concentration ranges from 0.6 to 300 μM. GSNOR activity for the oxidation of HMGSH by NAD+ is determined by measuring the increase in A340 due to reduction of NAD+ to NADH. An HMGSH stock solution is prepared by mixing methanol-free formaldehyde from sealed ampules and glutathione both to 30 mM in 100 mM sodium phosphate (pH 7.4). HMGSH concentrations for this stock solution and subsequent dilutions are calculated with a Keq for adduct dissociation of 1.77 mM. Kinetic constants are determined in 100 mM sodium phosphate buffer (pH 8.9) with a GSNOR concentration of 40 nM. For HMGSH constants, NAD+ is at a fixed concentration of 300 μM while the HMGSH concentration ranges from 0.003 to 44 μM. For the NAD+ constants, the HMGSH concentration is fixed at 83 μM and the NAD+ concentration ranges from 0.4 to 200 μM. Kinetic constants for all reactions are determined from a plot of the initial linear reaction rate versus substrate concentration and fit to a Michaelis–Menten model.
動物実験 動物モデル Mouse model of asthm.
投薬量 0.0005 to 30 mg/kg
投与方法 i.v. or p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

S-nitrosothiol homeostasis maintained by ADH5 facilitates STING-dependent host defense against pathogens [ Nat Commun, 2024, 15(1):1750] PubMed: 38409248
A histone deacetylase 3 and mitochondrial complex I axis regulates toxic formaldehyde production [ Sci Adv, 2023, 9(20):eadg2235] PubMed: 37196082
Vitamin C deficiency induces hypoglycemia and cognitive disorder through S-nitrosylation-mediated activation of glycogen synthase kinase 3β [ Redox Biol, 2022, 56:102420] PubMed: 35969998
Hiding in Plain Sight: Nebivolol Exhibits Compelling Tocolytic Properties [Barnett SD J Cell Mol Med, 2018, 22(12):6391-6395] PubMed: 30188599
S-Nitrosoglutathione Reductase Underlies the Dysfunctional Relaxation to Nitric Oxide in Preterm Labor. [ Sci Rep, 2018, 8(1):5614] PubMed: 29618799

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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