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Macitentan (Actelion-1,ACT-064992) CAS NO.441798-33-0
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Keywords
- macitentan
- CT-064992
- ACT064992
Quick Details
- ProName: Macitentan (Actelion-1,ACT-064992)
- CasNo: 441798-33-0
- Molecular Formula: C19H22Br2N6O4S
- Appearance: Off-white to white solid powder
- Application: Macitentan is an orally active, non-pe...
- DeliveryTime: Within 3-7 days after receipt of your ...
- PackAge: As customer request
- Port: Qingdao\Shanghai,China
- ProductionCapacity: 100 Kilogram/Week
- Purity: 99%
- Storage: Store in a cool,dry place and keep awa...
- Transportation: By Sea/Air/Courier
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Macitentan
[Synonyms]:N-[5-(4-Bromophenyl)-6-[2-[(5-Bromo-2-Pyrimidinyl)Oxy]Ethoxy]-4-Pyrimidinyl]-N'-Propylsulfamide
[Cas No]: 441798-33-0
[Molecular Formula]: C19H20Br2N6O4S
[Molecular Weight]: 588.27
[Specifications]:The Enterprise Standard ≥98%
[Package]:5kg/Tin,10kg/Tin
[Product Introduction]: White Or Almost White Crystalline Powder
[Use]:Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.
macitentan Chemical Properties
| density | 1.675 |
macitentan Usage And Synthesis
| Description | Macitentan (also known as ACT-064992) received US FDA approval in October 2013 for the treatment of pulmonary arterial hypertension (PAH) (WHO group I) to delay disease progression. Treatment options include phosphodiesterase type 5 inhibitors, prostacyclins, and the endothelin receptor antagonists bosentan and ambrisentan. Macitentan was discovered through SAR studies starting with the bosentan structure with three main goals: (1) to increase potency for both endothelin receptor A and B (ETA and ETB) subtypes; (2) to improve tissue distribution to reach the target receptors; and (3) to avoid bile salt transport inhibition. Starting with the bosentan sulfonamido-pyrimidinyl central core, potency was increased 10-fold via incorporation of a bromopyrimidinyl ethylene glycol ether, as found in the clinical endothelin antagonist, T-0201. An aryl ether in bosentan was replaced with the bromophenyl group in macitentan, and a substituent on the 2-position of the central pyrimidine was replaced with hydrogen. Several sulfonamides and alkyl sulfamates were explored, with the propylsulfamate providing the best combination of in vitro potency, especially for ETB antagonism, and in vivo efficacy. |
| Originator | Actelion Pharmaceuticals Ltd. (Switzerland) |
| Definition | ChEBI: A member of the class of sulfamides in which the two amino groups of sulfonamide are substituted by 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl and propyl groups. An orphan drug used for the treatment of pulmonary arterial hype tension. |
| Brand name | Opsumit |
