1414963-82-8
| 中文名称 | 1414963-82-8 |
|---|---|
| 中文同义词 | 1-(5-(呋喃-2-基)-1,3,4-恶二唑-2-基)-3-(吡啶-2-基甲基)脲;化合物NK-252 |
| 英文名称 | N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N′-(2-pyridinylmethyl)-urea |
| 英文同义词 | N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N′-(2-pyridinylmethyl)-urea;NK 252;NK252;Urea, N-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-N'-(2-pyridinylmethyl)-;NK-252 >=98% (HPLC);NK-252,NK252,NK 252,inhibit,Inhibitor,Keap1-Nrf2;1-(5-(Furan-2-yl)-1,3,4-oxadiazol-2-yl)-3-(pyridin-2-ylmethyl)urea |
| CAS号 | 1414963-82-8 |
| 分子式 | C13H11N5O3 |
| 分子量 | 285.26 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1414963-82-8.mol |
| 结构式 |  |
1414963-82-8 性质
| 密度 | 1.408±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 在DMSO中的溶解度为20mg/mL，澄清 |
| 酸度系数(pKa) | 11.50±0.70(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
Nrf2
The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 shows activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. NK-252 displays this effect with higher potency than OPZ based on the fact that the EC2 value (concentration for a 2-fold induction above background), calculated with linear extrapolation from the values above and below the induction threshold, is 20.8 μM for OPZ and 1.36 μM for NK-252. NK-252 has potential as an Nrf2 activator in hepatic cells. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H 2 O 2 -induced cytotoxicity. The protective effects of OPZ and NK-252 are examined against H 2 O 2 -induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H 2 O 2 -induced cytotoxicity compared with control cells.
Rats on a choline-deficient L-amino acid–defined (CDAA) diet given OPZ or NK-252 display decreased fibrosis scores compared with CDAA control rats, with median scores of 3, corresponding to bridging fibrosis. CDAA control rats display approximately 20-fold augmentation of the liver fibrosis area compared with rats fed a normal control diet (naive) (14.7 and 0.72%, respectively).This augmentation is also drastically reduced by administration of OPZ or NK-252 (5.80% for OPZ, 6.20% for NK-252_low, and 4.97% for NK-252_high). The effects of NK-252 on both fibrosis score and fibrosis area are dose-dependent. NK-252 alone has no antitumour effect in P388/S- and P388/VCR-mice. The combination therapy of Etoposide with NK-252 administered p.o. significantly increases the life-span of mice inoculated i.p. with P388/S compared with the corresponding therapeutic effects with Etoposide alone. The combination therapy with Etoposide and NK-252 significantly increases the life-span of mice inoculated i.p. with P388/VCR compared with the corresponding survival time with Etoposide alone.