99% Purity API Macitentan Powder CAS441798-33-0 Macitentan

Macitentan is a non-chiral sulfadiazine derivative. In vitro studies have shown that Macitentan is an oral antagonist of ETA
and ETB receptors, which can block endothelin-induced vasoconstriction in the trachea and aorta. Developed by Swiss Actelion
Pharmaceuticals and approved by the FDA on October 18, 2013, it was first listed in the United States, mainly for the treatment
of pulmonary hypertension (PAH), and its trade name is Opsumit. Compared with other drugs for PAH, macitentan can significantly
reduce the morbidity and mortality of PAH patients by slowing down the progress of the disease.

Works of Dasatinib Powder

Maxititan is a new type of dual endothelin receptor antagonist for oral ETRA and ETRB. Maxititan is metabolized to
ACT-132577 through CYP3A4 in vivo. Both of them inhibit the binding of ET-1 to ETA and ETB. In an in vitro receptor
selection and functional blocking test, the IC50 of mecitentan blocking ETA and ETB were (0.5 + 0.2) nmol.L-1 (n = 17)
and (391 + 182) nmol.L-1 (n = 17), respectively, and the IC50 of ACT-132577 to ETA and ETB were (3.4 + 0.4) nmol.L
-1 (n = 4) and (987 + 185) nmol.L-1 (n = 9). Marcetitan and ACT-132577 can prevent ET-1 from binding to ETA and ETB
receptors, further preventing ET-1-induced intracellular calcium increase and vasoconstriction.

In DOC (deoxycorticosterone acetate) salt hypertensive rats, single dose of 10 mg of maxitian can reduce arterial blood
pressure (26 +4) mmHg, and single dose of 100 mg of bosentan can reduce arterial blood pressure (20 +5) mmHg. Both
of them have no effect on heart rate. Mecitentan can cause the same or even better hypotensive effect when its concentration
is 10 times lower than that of bosentan, and the lasting time of mecitentan is bosen. The pharmacological activity of mecitentan
was 2 times higher than that of bosentan.

Macitentan lowers blood pressure in your lungs, helping your heart pump blood more efficiently.

Macitentan is used to treat pulmonary arterial hypertension (PAH). It improves your ability to exercise and prevents your
condition from getting worse.

Macitentan is available to women only under a special program from a certified pharmacy. You must be registered in the
program and understand the risks and benefits of taking this medication.



Macitentan was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension and is marketed
under the brand name Opsumit. Macitentan is an antagonist/blocker of endothelin receptors on blood vessels and smooth
muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction.
Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should
not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age.