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macitentan

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441798-33-0 Basic informationMore
USE
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<sub>A</sub> and ET<sub>B</sub>) 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.
Lastest Price from macitentan manufacturers
  • Macitentan
  • US $0.00 /KG
  • CAS:441798-33-0
  • Min. Order: 1KG
  • Purity: 99%min
  • Supply Ability: 100kg
  • 2023-11-15
  • macitentan
  • US $0.00 /KG
  • CAS:441798-33-0
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 50000KG/month
  • 2023-06-29

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  • Company Name:Anhui Qiushi Medical Technology Co., Ltd
  • Tel: 15005516438
  • Products Intro:Product Name:macitentan
    CAS:441798-33-0
    Purity:99%;医药级 Package:10kg
  • CB Index:58
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  • Company Name:Hangzhou XunDa Bio-Technology Co., Ltd.
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    Purity:99% Package:25kg More...
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  • Company Name:Chengdu Climb Pharmaceutical Technology Co., Ltd.
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  • Tel:0576-0576-89232655 13566878689
  • Products Intro:Product Name:macitentan; N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide
    CAS:441798-33-0
    Purity:99%HPLC Package:克至百公斤级以上 More...
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  • Company Name:J & K SCIENTIFIC LTD.
  • Tel:010-82848833 400-666-7788
  • Products Intro:Product Name:Macitentan
    CAS:441798-33-0
    Package:100Mg,25Mg,5Mg More...
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  • Company Name:Chembest Research Laboratories Limited
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  • Products Intro:Product Name:N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N-propylsulfamide
    CAS:441798-33-0
    Purity:98% HPLC Package:5g;10g Remarks:Biochemical Reagents; Pharmaceutical Intermediates More...
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  • Company Name:BeiJing Hwrk Chemicals Limted
  • Tel:0757-86329057 18501085097
  • Products Intro:Product Name:macitentan
    CAS:441798-33-0
    Purity:95.00% Package:1g
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