您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > MRS 2578
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：
 
MRS 2578
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。
MRS 2578图片
CAS NO:711019-86-2
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
MRS 2578 是一种选择性有效的 P2Y6 受体拮抗剂，IC50 为 37 nM（人）和 98 nM（大鼠）。
Cas No.711019-86-2
化学名1-(3-isothiocyanatophenyl)-3-[4-[(3-isothiocyanatophenyl)carbamothioylamino]butyl]thiourea
Canonical SMILESC1=CC(=CC(=C1)NC(=S)NCCCCNC(=S)NC2=CC=CC(=C2)N=C=S)N=C=S
分子式C20H20N6S4
分子量472.68
溶解度≥ 19.75mg/mL in DMSO
储存条件Store at 2-8℃
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

MRS 2578 is a potent and insurmountable antagonist of P2Y6 nucleotide receptor with IC50 value of 37nM [1].

MRS 2578, a diisothiocyanate derivative, is an insurmountable antagonist of P2Y6 receptors which are associated with vasoconstriction. Thus MRS 2578 is expected to be used in treatment of vasospasm. In 1321N1 human astrocytes expressing P2Y6 receptors, MRS 2578 inhibits the UDP-induced accumulation of inositol phosphates in a dose-dependent manner. MRS 2578 also inhibits the rat P2Y6 receptor activation with IC50 value of 98nM. These effects are selective. MRS 2578 has no effect on the UTP-induced responses of cells expressing human P2Y2 or P2Y4 receptors. It also has no effect on the 2-MeSADP-induced responses of cells expressing the P2Y1 receptor. Moreover, since the UDP-induced activation of P2Y6 receptor can protect the cells from apoptosis induced by TNFα, MRS 2578 completely blocks the protection of cells [1].

References:
[1] Mamedova L K, Joshi B V, Gao Z G, et al. Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors[J]. Biochemical pharmacology, 2004, 67(9): 1763-1770.