| 產(chǎn)品描述： | N6022(IC50 of 8 nM) is an effective, reversible, and selective S-Nitrosoglutathione reductase(GSNOR) inhibitor. |
| 靶點(diǎn)： |
GSNOR |
| 體外研究： |
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. |
| 體內(nèi)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. |
| 細(xì)胞實(shí)驗(yàn)： |
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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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