CAS: 175556-12-4

(R)-4-(tert-Butyl)-N-(6-(2,3-dihydroxypropoxy)-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)pyrimidin-4-yl)benzenesulfonamide is a non-peptide antagonist of endothelin A (ET A ) and endothelin B (ET B ). It has been shown to have a high selectivity for ET A over ET B , with potency at concentrations of 1 nM for ET A and 100 nM for ET B . This compound has been shown to inhibit the release of vasoconstrictive endothelin from cultured human endothelial cells. The inhibition is concentration dependent, with shifts in the concentration-response curves being observed as low as 10 μM. The inhibition of release was characterised by clarifying the mechanism involved.

RO 46-8443

RO 46-8443: First non-peptide ETB receptor antagonist, >2000-fold ETB selectivity in binding and function.