||Ambrisentan is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme eleva
||Macitentan is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension (PAH).
||Ro 46-2005 is a synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor, IC50: 220 nM).
||RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibit
||Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.
||Bosentan is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor.
||Bosentan is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.
||Sitaxsentan (sodium) is a highly selective antagonist of endothelin A receptors.
||BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
||Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries
||Aprocitentan is ETA and ETB antagonist .
||Atrasentan (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).
||Atrasentan hydrochloride (ABT-627 hydrochloride) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).
||Avosentan (Ro 67-0565) is an effective and selective antagonist of the endothelin receptor (ETA receptor).
||Myriceric acid C
||Myriceric acid C has cytotoxic activity against human lung carcinoma and breast carcinoma.
||Sparsentan is a first-in-class orally active and highly potent dual endothelin A and angiotensin II receptor antagonist(Ki of 9.3 and 0.8 nM, respectively)