Ambrisentan

CAS: 177036-94-1

MF: C22H22N2O4

MW: 378.42

EINECS: 658-059-9

Melting point >150°C (dec.)

Boiling point 551.1±60.0 °C(Predicted)

density 1.228±0.06 g/cm3(Predicted)

storage temp. -20°C Freezer

Ambrisentan is a selective endothelin-A (ETA) receptor antagonist introduced for the oral treatment of patients with pulmonary arterial hypertension (PAH), to improve exercise capacity and delay clinical worsening. It is the third ET-receptor antagonist to be marketed for this indication behind bosentan and sitaxsentan. PAH is a rare disease of the small pulmonary arteries characterized by vascular proliferation and remodeling, resulting in a progressive increase in pulmonary vascular resistance and pulmonary arterial pressure, and ultimately, right ventricular failure and premature death. Early symptoms of PAH include gradual onset of shortness of breath, fatigue, palpitation, edema, and fainting. Endothelin-1 (ET-1), a potent vasoconstrictor and smooth muscle mitogen, is a key contributor to the acceleration of the disease, and its effects are mediated through activation ofETA and ETB receptors.