1414963-82-8
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- CAS号:
- 1414963-82-8
- 英文名:
- N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N′-(2-pyridinylmethyl)-urea
- 英文别名:
- NK 252;NK252;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;N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N′-(2-pyridinylmethyl)-urea;Urea, N-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-N'-(2-pyridinylmethyl)-
- 中文名:
- 1414963-82-8
- 中文别名:
- 化合物NK-252;1-(5-(呋喃-2-基)-1,3,4-恶二唑-2-基)-3-(吡啶-2-基甲基)脲
- CBNumber:
- CB72750704
- 分子式:
- C13H11N5O3
- 分子量:
- 285.26
- MOL File:
- 1414963-82-8.mol
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1414963-82-8化学性质
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密度:
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1.408±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble20mg/mL, clear
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酸度系数(pKa):
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11.50±0.70(Predicted)
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形态:
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powder
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颜色:
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white to beige
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1414963-82-8性质、用途与生产工艺
NK-252 是一种潜在的 Nrf2 激活剂，具有很好的 Nrf2 活化能力。
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.
1414963-82-8
上下游产品信息
上游原料
下游产品
1414963-82-8, 1414963-82-8 相关搜索:
- 化合物NK-252
- 1-(5-(呋喃-2-基)-1,3,4-恶二唑-2-基)-3-(吡啶-2-基甲基)脲
- 1414963-82-8
- 1-(5-(Furan-2-yl)-1,3,4-oxadiazol-2-yl)-3-(pyridin-2-ylmethyl)urea
- NK-252,NK252,NK 252,inhibit,Inhibitor,Keap1-Nrf2
- NK-252 >=98% (HPLC)
- Urea, N-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-N'-(2-pyridinylmethyl)-
- NK 252;NK252
- N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N′-(2-pyridinylmethyl)-urea