Home GPCR & G Protein Endothelin Receptor ET-A Selective Antagonists

ET-A Selective Antagonists

  • ET-A
  • ET-B
Catalog No. Product Name Information Selective / Pan IC50 / Ki
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