首页 蛋白库 基因库 产品 会员服务
位置：首页 > 产品库 > S18886
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：
 
S18886
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。
S18886图片
CAS NO:165538-40-9
包装与价格：
包装价格(元)
5mg询价
10mg询价

S18886 是一种血栓素-前列腺素受体拮抗剂。
Cas No.165538-40-9
别名特鲁曲班,Terutroban,Triplion
化学名(6R)-6-[[(4-chlorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydro-2-methyl-1-naphthalenepropanoic
Canonical SMILESCC1=C(CCC(O)=O)C2=C(C=C1)C[C@H](NS(C3=CC=C(Cl)C=C3)(=O)=O)CC2
分子式C20H22ClNO4S
分子量407.9
溶解度≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/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

IC50: 16.4 nM for TP receptor

S18886 is a potent thromboxane A2 (TP) inhibitor.

The lipid mediator thromboxane A2 (TXA2) plays a critical role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated via the specific G protein coupled-receptor, TXA2 receptor (TP).

In vitro: S18886 was identified as the active isomer of the potent TP receptor antagonist S18204. S18886 was also found to be a selective antagonist of thromboxaneprostaglandin receptors in platelets and in the vessel wall [1].

In vivo: In a previous animal study, it was found that S18886 treatment could reduce the portal pressure in both animal models without producing significant changes in portal blood flow, indicating a reduction in hepatic vascular resistance. S18886 could not significantly change arterial pressure in CCl4 -cirrhotic rats but could significantly decrease it in BDL-cirrhotic rats [2].

Clinical trial: A previoius trial aiming to evaluate S18886 versus aspirin in patients with cerebral ischaemic events showed similar rates of the primary endpoint with S18886 and aspirin, without safety advantages for S18886 [3].

References:
[1] Cimetière B, Dubuffet T, Landras C, Descombes JJ, Simonet S, Verbeuren TJ, Lavielle G.  New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors. Bioorg Med Chem Lett. 1998 Jun 2;8(11):1381-6.
[2] Rosado E, Rodríguez-Vilarrupla A, Gracia-Sancho J, Tripathi D, García-Calderó H, Bosch J, García-Pagán JC.  Terutroban, a TP-receptor antagonist, reduces portal pressure in cirrhotic rats. Hepatology. 2013 Oct;58(4):1424-35.
[3] Bousser MG, Amarenco P, Chamorro A, Fisher M, Ford I, Fox KM, Hennerici MG, Mattle HP, Rothwell PM, de Cordoüe A, Fratacci MD; PERFORM Study Investigators. Terutroban versus aspirin in patients with cerebral ischaemic events (PERFORM): a randomised, double-blind, parallel-group trial. Lancet. 2011 Jun 11;377(9782):2013-22.

 
 
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024