Endothelin Receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1456 Zibotentan (ZD4054) <1 mg/mL 24 mg/mL <1 mg/mL
S3051 Bosentan Hydrate 0.001 mg/mL 100 mg/mL 2 mg/mL
S8051 Macitentan <1 mg/mL 100 mg/mL <1 mg/mL
S2097 Ambrisentan <1 mg/mL 76 mg/mL 22 mg/mL
S7883 BQ-123 <1 mg/mL 100 mg/mL 15 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

Zibotentan (ZD4054)

Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.


Bosentan Hydrate

Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.



Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.



Ambrisentan is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).



BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.