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Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist

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Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist

China Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist supplier
Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist supplier Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist supplier

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Place of Origin: Weifang,China
Brand Name: RuzE
Model Number: TC-9030

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Minimum Order Quantity: Negotiable
Price: Negotiable
Packaging Details: 10g
Delivery Time: 5-10workdays
Payment Terms: L/C, T/T, , Western Union, MoneyGram
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Detailed Product Description
Product Name: Macitentan CAS: 441798-33-0
MF: C19H22Br2N6O4S MW: 590.295
EINECS: 1308068-626-2 Mol File: 441798-33-0.mol

Weifang Ruze New Material Co.,LTD a China supplier of N-[5-(4-Bromophenyl)-6-[2-[(5-Bromo-2-Pyrimidinyl)Oxy]Ethoxy]-4-Pyrimidinyl]-N'-Propylsulfamide(CAS No.:441798-33-0 ),CAS 441798-33-0 offers for your requirements of RND, evaluation, pilots and commercial along with supportive technical package required for evaluation.

Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist

 

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
 
 

Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor AntagonistMacitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist

Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor AntagonistMacitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor AntagonistMacitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist

 

Macitentan CAS:441798-33-0 Antineoplastic Drugs Dual ETA / ETB Receptor Antagonist

Weifang Ruze New Material Co.,LTD supply free sample and datebase on N-[5-(4-Bromophenyl)-6-[2-[(5-Bromo-2-Pyrimidinyl)Oxy]Ethoxy]-4-Pyrimidinyl]-N'-Propylsulfamide(CAS No.:441798-33-0 ), if you want futher information about N-[5-(4-Bromophenyl)-6-[2-[(5-Bromo-2-Pyrimidinyl)Oxy]Ethoxy]-4-Pyrimidinyl]-N'-Propylsulfamide(CAS No.:441798-33-0 ), please feel free to contract us.

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