S80170 |
N6022 |
源叶(MedMol) | 98% |
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- 产品描述: N6022(IC50 of 8 nM) is an effective, reversible, and selective S-Nitrosoglutathione reductase(GSNOR) inhibitor.
- 靶点: GSNOR
- 体外研究:
N6022 binds to rat plasma proteins in a concentration-dependent manner. At lower drug concentrations (20 μM), N6022 show more effect on ATP than on GSH. N6022 (IC50 of 8 nM and a Ki of 2.5 nM) binds in the GSNO substrate binding pocket like a competitive inhibitor. N6022 is uncompetitive with cofactors NAD+ and NADH.
- 体内研究:
N6022 treats rats in 50 mg/kg leading to a slight increase in the incidence of granulomas. In serum, N6022 remained in solution is up to 5 mg/mL.
- 细胞实验: N6022 is dissolved in 5% DMSO. N6022 is tested using a rat hepatoma (H4IIE) cell line whereby cells are seeded into 96-well plates and cultured in medium containing 20% bovine serum. Following an equilibration period of 48 h, the cells are treated with N6022 (5% DMSO vehicle) at concentrations of 0, 1, 5, 10, 20, 50, 100, and 300 μM for 24 h at 37°C in 5% CO2. Camptothecin and rotenone are included as positive controls. The cell supernatant or the cells themselves are harvested for biochemical analysis.
- 参考文献:
1. Green LS, et al. Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. Biochemistry. 2012, 51(10), 2157-2168 2. Sun X, et al. Discovery of s-nitrosoglutathione reductase inhibitors: potential agents for the treatment of asthma and other inflammatory diseases. ACS Med Chem Lett. 2011, 2(5), 402-406.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.413 ml 12.064 ml 24.128 ml 5 mM 0.483 ml 2.413 ml 4.826 ml 10 mM 0.241 ml 1.206 ml 2.413 ml 50 mM 0.048 ml 0.241 ml 0.483 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)