您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > NK-252
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
NK-252
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NK-252图片
CAS NO:1414963-82-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
NK-252 是潜在的Nrf2激活剂,具有很好的Nrf2活化活性。

产品描述

NK-252 is a potential activator of Nrf2. It has great Nrf2-activating potential.

体外活性

NK-252 shows 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. 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. The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 displays activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H2O2-induced cytotoxicity [1].

体内活性

Rats on a choline-deficient L-amino acid–defined (CDAA) diet given OPZ or NK-252 show decreased fibrosis scores compared with CDAA control rats. The effects of NK-252 on both fibrosis score and fibrosis area are dose-dependent[1]. Compared with rats fed a normal control diet (naive) (14.7 and 0.72%, respectively), CDAA control rats display approximately 20-fold augmentation of the liver fibrosis area. 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). NK-252 alone has no antitumor effect in P388/S- and P388/VCR-mice. 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[2]. 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.

Cas No.

1414963-82-8

分子式

C13H11N5O3

分子量

285.26

储存和溶解度

DMSO:29 mg/mL (101.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years