CasNo.441798-33-0,Macitentan (Actelion-1,ACT-064992),(441798-33-0) Suppliers

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Purity: 99%
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Keywords

macitentan CT-064992 ACT064992

Quick Details

Appearance:Off-white to white solid powder
Application:Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.
PackAge:As customer request
ProductionCapacity:100|Kilogram|Week
Storage:Store in a cool,dry place and keep away from direct strong light
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 (ET_A and ET_B) 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