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1414963-82-8

中文名稱(chēng) 1414963-82-8
英文名稱(chēng) N-[5-(2-Furanyl)-1,3,4-oxadiazol-2-yl]-N′-(2-pyridinylmethyl)-urea
CAS 1414963-82-8
分子式 C13H11N5O3
分子量 285.26
MOL 文件 1414963-82-8.mol
更新日期 2024/11/01 22:00:07
1414963-82-8 結(jié)構(gòu)式 1414963-82-8 結(jié)構(gòu)式

基本信息

中文別名
化合物NK-252
1-(5-(呋喃-2-基)-1,3,4-惡二唑-2-基)-3-(吡啶-2-基甲基)脲
英文別名
NK 252
NK252
NK-252 >=98% (HPLC)
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)-

物理化學(xué)性質(zhì)

密度1.408±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL,澄清
酸度系數(shù)(pKa)11.50±0.70(Predicted)
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
防范說(shuō)明P280-P305+P351+P338
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類(lèi)別碼22
WGK Germany3

常見(jiàn)問(wèn)題列表

生物活性
NK-252 是一種潛在的 Nrf2 激活劑,具有很好的 Nrf2 活化能力。
靶點(diǎn)

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 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.

體內(nèi)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.

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