| S6665 |
Sparsentan (PS-433540, RE-021) |
Sparsentan (PS-433540, RE-021, DARA) is a dual endothelin type A receptor(ETA) and angiotensin II type 1 receptor antagonist. |
Selective |
|
| S0017 |
Lu-135252 |
Lu-135252 (Darusentan,HMR-4005) is a selective endothelin A receptor (ET-A receptor) antagonist indicated for the oral treatment of resistant hypertension. |
Selective |
|
| S8051 |
Macitentan (ACT 064992) |
Macitentan (ACT 064992) is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM. |
Selective |
ET-A, IC50: 0.5 nM |
| S3051 |
Bosentan Hydrate |
Bosentan (Ro 47-0203) is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
Selective |
ET-A, Ki: 4.7 nM |
| S7883 |
BQ-123 |
BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
|
Selective |
Endothelin A receptor, IC50: 7.3 nM |
| S1456 |
Zibotentan (ZD4054) |
Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3. |
Selective |
ET-A, IC50: 21 nM |
| S2097 |
Ambrisentan |
Ambrisentan (LU-208075, BSF-208075) is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH). |
Selective |
|
