產品描述: N6022(IC50 of 8 nM) is an effective, reversible, and selective S-Nitrosoglutathione reductase(GSNOR) inhibitor. |
靶點:
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. |
細胞實驗:
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:
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: |
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