Macitentan（Cat No.:A000156）is an endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). By selectively blocking both endothelin receptor subtypes, ETA and ETB, it prevents endothelin-1 from causing vasoconstriction and vascular remodeling, which are key contributors to PAH. This results in improved blood flow, reduced pulmonary pressure, and enhanced exercise capacity. Macitentan is designed to provide long-lasting effects with a reduced risk of liver toxicity compared to earlier drugs in its class, making it a preferred option for managing PAH and improving patient outcomes.
| Catalog Number | A000156 |
| CAS Number | 441798-33-0 |
| Synonyms | ACT 064992; Opsumit |
| Molecular Formula | C19H20Br2N6O4S |
| Purity | ≥95% |
| Target | Endothelin Receptor |
| Solubility | >21.2mg/mL in DMSO |
| Storage | 3 years, -20°C |
| Overview of Clinical Research | Macitentan is an endothelin A receptor antagonist and endothelin B receptor antagonist developed by Actelion Pharmaceuticals. |
| IUPAC Name | 5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine |
| InChI | InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27) |
| InChIKey | JGCMEBMXRHSZKX-UHFFFAOYSA-N |
| SMILES | CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br |
