ET_A Inhibitor

S-1255 is an orally active and highly selective endothelin ETA receptor antagonist (K_d=0.39 nM). S-1255 blocks vasoconstriction and sustains hypotensive effects in hypertensive rats. S-1255 is promising for research of hypertension and cardiovascular disorders.

PD 155080 is a selective endothelin A receptor (ET_A receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases.

Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan sodium is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan sodium exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.