| CAS NO: | 1103522-45-7 |
| 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 |
| 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 SMILES | BrC1=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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: |
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