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 > AZ 11645373
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:
 
AZ 11645373
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。
AZ 11645373图片
CAS NO:227088-94-0
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Human P2X7 antagonist,potent and selective
Cas No.227088-94-0
别名3-{1-[(3'-硝基-4-联苯基)氧基]-4-(4-吡啶基)-2-丁烷基}-1,3-噻唑烷-2,4-二酮
化学名(R)-3-(1-((3'-nitro-[1,1'-biphenyl]-4-yl)oxy)-4-(pyridin-4-yl)butan-2-yl)thiazolidine-2,4-dione
Canonical SMILESO=C1N(C(SC1)=O)[C@@H](COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC4=CC=NC=C4
分子式C24H21N3O5S
分子量463.51
溶解度<4.64mg/ml in DMSO
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

AZ11645373 is identified as a highly selective and potent antagonist of human P2X7 receptors but not mouse/rat P2X7 receptors.

Adenosine 5′-triphosphate (ATP)-gated P2X receptors (P2XRs) comprise of seven genes which encode plasma membrane ion channels for calcium cation. These proteins are differentially expressed throughout autonomic, sensory and central neurons as well as in visceral smooth muscle, epithelia and immune cells. P2XRs was also reported to have potential roles in acute and/or chronic pain sensation.

In cellular culture, treatment of AZ11645373 inhibited human P2X7 receptor responses in HEK cells, which dislayed in a non-surmountable manner with K B values ranging from 5 - 20 nM 1. K B values were not altered by removing extracellular calcium and magnesium. In addition, AZ11645373 treatment inhibited ATP-evoked IL-1β release from lipopolysaccharide- activated THP-1 cells with IC50 = 90 nM 1.

Regarding the effect of AZ11645373 administration in vivo, the evidence should be provided by performing the study in human or mice or other animal models.

Reference:
1.  Stokes L, Jiang LH, Alcaraz L, et al. Characterization of a selective and potent antagonist of human P2X(7) receptors, AZ11645373. British journal of pharmacology. 2006;149(7):880-887.