| 貨號 | 規格 | 價格 | 上海 | 北京 | 武漢 | 南京 | 購買數量 |
|---|---|---|---|---|---|---|---|
S83171-5mg |
99.7% | ￥500.00 | 3 | - | - | - |
|
S83171-10mg |
99.7% | ￥800.00 | 5 | - | - | - |
|
S83171-25mg |
99.7% | ￥1600.00 | 5 | - | - | - |
|
S83171-100mg |
99.7% | ￥4800.00 | 1 | - | - | - |
|
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
| 產品描述： | NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點： | Nrf2;Others;?Nrf2 | ||||||||||||||||||||
| 體外研究： | 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 H2O2-induced cytotoxicity. The protective effects of OPZ and NK-252 are examined against H2O2-induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H2O2-induced cytotoxicity compared with control cells. | ||||||||||||||||||||
| 體內研究： | 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. | ||||||||||||||||||||
| 參考文獻： | 1. Shimozono R et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul, 84(1):62-70. 2. Kiue A, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6. | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存條件： | -20℃ | ||||||||||||||||||||
| 配置溶液濃度參考： |
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| 注意： | 部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
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危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京