Macitentan(ACT-064992)

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Chemical Information

Product name：Macitentan(ACT-064992)	Purity：98% min
CAS NO：441798-33-0	Solubility：DMSO: 100 mg/mL (169.98 mM)
Molecular Formula：C₁₉H₂₀Br₂N₆O₄S	Package：Package according to customer requirements
Molecular Weight：588.27	Storage：Store at -20℃

Quality control

COA

Remarks

Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH). The other two ERAs marketed as of 2014 are bosentan and ambrisentan. Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype. The drug received approval from the U.S. Food and Drug Administration (FDA) on October 13, 2013.

Endothelin Receptor Inhibitors Related Prodcuts:

Bosentan; Bosentan hydrate; Ambrisentan; Sparsentan; Zibotentan

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.