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Postion:Product Catalog >Pharmaceutical intermediates>Bulk Drug Intermediates>macitentan
macitentan
  • macitentan
  • macitentan

macitentan

Price Get Latest Price
Package 5KG 10KG 20KG
Min. Order: 1KG
Supply Ability: 300kgs
Update Time: 2023-04-20

Product Details

Product Name: macitentan CAS No.: 441798-33-0
Min. Order: 1KG Purity: 99.9% HPLC; USP42
Supply Ability: 300kgs Release date: 2023/04/20

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.



Company Profile Introduction

Hefei Tianrui Pharmaceutical Chemical Co., Ltd. is located in the Industrial Park of Huagang Town, Feixi County, Hefei City. With excellent R&D capabilities, a complete set of complementary industrialization support, and an international CGMP quality management system, Tianrui is committed to providing professional technical services and commercialization of small molecule specialty APIs, CGMP standard intermediates, functional pharmaceutical excipients, and MRNA vaccine vectors for domestic and overseas well-known pharmaceutical enterprises. The company has independently developed and commercialized a range of new drug products, including Roflumilast, Rivaroxaban, Ezetimibe, Dasatinib, Repaglinide, Prucalopride Succinate, Salcaprozate sodium (8-(2-hydroxybenzamido)octanoate), Vandetanib, Garenoxacin, Ropinirole hydrochloride, Conivaptan hydrochloride, Crizotinib, Olaparib, Macitentan, Difamilast, Tepotinib, Tanimilast, Foscarbidopa, etc. Among them, Salcaprozate sodium (8-(2-hydroxybenzamido)octanoate) has successfully obtained registration numbers from both the Chinese CDE and the US FDA (CDE registration number: F20220000072; USDMF number: 037135). Meanwhile, we also have strength of long chain intermediates such as 8-Bromooctanoic Acid, 8-Aminooctanoic Acid, Methyl 8-bromooctanoate, Ethyl 8-bromooctanoate, 6-Bromohexanoic Acid, Ethyl 7-bromooctanoate, Diphenyl Phosphate, Tetrabenzyl pyrophosphate, 4-(Boc-Amino)cyclohexanone, etc. The products are mainly exported to Europe, North America, India, Japan, Korea and other countries, and we can provide the documentation support and audit requirements of the said corresponding regulatory markets. Tianrui Pharmaceutical is dedicated to the lifelong mission of striving for human health, continuously updating excellent products and services, and making contributions to breaking through the global barriers in the pharmaceutical industry.

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