您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > EA4
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:
 
EA4
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。
EA4图片
CAS NO:389614-94-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Cas No.389614-94-2
化学名7-chloro-6-[4-(diethylamino)phenyl]-5,8-quinolinedione
Canonical SMILESCCN(CC)c1ccc(cc1)C1=C(Cl)C(=O)c2ncccc2C1=O
分子式C19H17ClN2O2
分子量340.8
溶解度≤1mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki: 130 μM

EA4 is a rPLA2 inhibitor.

rPLA2, a calcium-dependent cytosolic phospholipase A2 (cPLA2), was initially isolated and characterized from bovine and human red blood cells. With a molecular mass of 42 kDa, cPLA2 shows biochemical properties similar to cPLA2 Type IV.

In vitro: It was found that EA4 was able to inhibit a Ca(2+) ionophore-induced arachidonic acid release from both human and bovine red blood cells, demonstrating that this enzyme was responsible for the Ca(2+)-dependent arachidonic acid release from mammalian red blood cells [1]. Another study found that in mouse hepatoma Hepa-1c1c7 cells, EA4 could cause a significant induction of the CYP1A1-mediated ethoxyresorufin O-deethylase activity time- and concentration-dependently, and such induction was accompanied by an increase of the Cyp1a1 mRNA transcription. Morevoer, in human cells including MCF-7 (human breast adenocarcinoma cell line), HepG2 (human hepatocarcinoma), and HL-60 (human promyelocytic cell line), the expression of CYP1A1 mRNA could be also induced by EA4 treatment. In addition, CYP1B1 mRNA was increased by EA4 in MCF-7 cells [2].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

References:
1.  Shin, H.S.,Chin, M.R.,Kim, J.S., et al. Purification and characterization of a cytosolic, 42-kDa and Ca2+-dependent phospholipase A2 from bovine red blood cells. The Journal of Biological Chemisty 277, 21086-21094 (2002).
2.  Chun, Y.J.,Lee, B.Y.,Yang, S.A., et al. Induction of cytochrome P450 1A1 gene expression by a vitamin K3 analog in mouse hepatoma Hepa-1c1c7 cells. Molecules and Cells 12, 190-196 (2001).