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ACT-132577
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。
ACT-132577图片
CAS NO:1103522-45-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
ACT-132577 (ACT-132577) 是 Macitentan 的主要且具有药理活性的代谢物。
Cas No.1103522-45-7
别名N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺,ACT-132577
Canonical SMILESBrC1=CC=C(C2=C(OCCOC3=NC=C(Br)C=N3)NC=N/C2=N\S(N)(=O)=O)C=C1
分子式C16H14Br2N6O4S
分子量546.19
溶解度Soluble 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

ACT-132577 is a dual antagonist of ETA and ETB receptors with IC50 values of 3.4nM and 987nM, respectively [1].

ACT-132577 is a major metabolite of macitentan which is a dual ET receptor antagonist with strong affinity for the tissues. Macitentan is metabolized into ACT-132577 in vivo. ACT-132577 is also a dual ET receptor antagonist and has a longer half-life than its parent compound. In assays using microsomal membranes of CHO cells overexpressing human ETA and ETB receptors, ACT-132577 shows potent effects on ETA and ETB receptors with IC50 values of 3.4nM and 987nM, respectively. In the in vitro functional assay, ACT-132577 completely inhibits the intracellular calcium increase induced by ET-1with IC50 values of 14nM, 5.8nM and 10.9nM in HPASMC, RASMC and m3T3 cells, respectively. ACT-132577 also causes a significant reduction of sarafotoxin S6c-induced contraction in isolated rat trachea [1].

In normotensive rats, administration of macitentan increases plasma ET-1 concentration. In hypertensive DOCA-salt rats, macitentan decreases mean arterial blood pressure. Besides that, macitentan suppresses the development of pulmonary hypertension and right ventricle hypertrophy in the monocrotaline model of pulmonary hypertension as well as in the streptozotocin model of diabetes [1].

References:
[1] Iglarz M, Binkert C, Morrison K, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. Journal of Pharmacology and Experimental Therapeutics, 2008, 327(3): 736-745.