Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Macitentan
Price:
Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Macitentan
Price: ￥928.0/1g ￥248.0/1g
Purity: 99.0%
Stocking Period: 1 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: Macitentan (Actelion-1,ACT-064992)
Price: $250.0/100mg $400.0/250mg $800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

ShangHai DC Chemicals Co.,Ltd
China
Product Name: Macitentan (Actelion-1,ACT-064992)
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai

Henan Tianfu Chemical Co., Ltd.
China
Product Name: macitentan
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

441798-33-0

441798-33-0 structure

441798-33-0 structure

Name: Macitentan
Chemical Name: macitentan
CAS Number: 441798-33-0
Molecular Formula: C₁₉H₂₀Br₂N₆O₄S
Molecular Weight: 588.27
Catalog: Pharmaceutical intermediate API intermediate
Create Date: 2018-09-17 12:03:12
Modify Date: 2024-01-02 08:09:19
Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.

Name	macitentan
Synonyms	5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine Macitentan Actelion-1 Opsumit N-[5-(4-Bromophenyl)-6-{2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy}-4-pyrimidinyl]-N'-propylsulfuric diamide Sulfamide, N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propyl- ACT-064992 N-[5-(4- bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)- pyrimidin-4-yl]-N-propylaminosulfonamide

Description	Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor Research Areas >> Cardiovascular Disease
In Vitro	Tube formation ability is restored when microvascular endothelial cells are preincubated with BOS or macitentan, also reducing the expression of mesenchymal markers and restoring CD31 expression and the imbalance between VEGF-A and VEGF-A165b[1]. Macitentan inhibits OATP1B1-mediated uptake of atorvastatin and OATP1B3-mediated uptake of estrone-3-sulfate with IC50 ± SE values of 6.3 ± 0.7 and 11.8 ± 5.0 μM, respectively[3]. Treatment with macitentan or with ACT-132577 does not lead to intracellular accumulation of R123 in HeyA8-MDR, showing that these compounds are not P-gp inhibitors[4].
In Vivo	Macitentan (25 mg/kg/day, p.o.) prevents increased production of vasoactive and fibrogenic factors, NF-κB activation, structural and functional changes, and increases extracellular matrix protein production in type 2 diabetes in type 2 diabetes[2]. Macitentan (10 mg/kg, p.o.) coupled with once-per-week 5 mg/kg taxol, significantly reduces the weight (size) of HeyA8-MDR tumors in mice. Combination therapy with macitentan (10 or 50 mg/kg, but not 5 mg/kg) and taxol or macitentan (10 mg/kg) and cisplatinum significantly reduces the number of proliferating Ki-67-positive cells[4].
Animal Admin	Male db/db mice and age and sex-matched controls (27-32 g) are used for the assay. RandomLy selected diabetic animals are monitored for either 2 months or for 4 months after onset of diabetes. Groups (n=7/group) of the diabetic mice are subjected to oral macitentan treatment for the same period (25 mg/kg/day, food admix). The animals are monitored through assessment of body weight and blood glucose.
References	[1]. Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18(1):228. [2]. Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Apr 13. [3]. Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14(1):68-78. [4]. Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist.Transl Oncol. 2012 Feb;5(1):39-47.

Density	1.7±0.1 g/cm3
Boiling Point	692.4±65.0 °C at 760 mmHg
Molecular Formula	C₁₉H₂₀Br₂N₆O₄S
Molecular Weight	588.27
Flash Point	372.5±34.3 °C
PSA	159.84000
LogP	5.41
Vapour Pressure	0.0±2.2 mmHg at 25°C
Index of Refraction	1.634
Storage condition	-20℃

Hazard Codes	Xi