Endothelin Receptor

Sigaling 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
S3034 Sitaxentan sodium <1 mg/mL 40 mg/mL 20 mg/mL
S2097 Ambrisentan <1 mg/mL 76 mg/mL 22 mg/mL
S4220 Bosentan <1 mg/mL 100 mg/mL 3 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
S1456

Zibotentan (ZD4054)

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

S3051

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.

S8051

Macitentan

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

S3034

Sitaxentan sodium

Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3.

S2097

Ambrisentan

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

S4220

Bosentan

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

S7883

BQ-123

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

Catalog No. Information Product Use Citations Product Validations
S1456

Zibotentan (ZD4054)

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

2016, 63(3):1000-12

S3051

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.

S8051

Macitentan

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

S3034

Sitaxentan sodium

Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3.

S2097

Ambrisentan

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

S4220

Bosentan

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

2016, 11(9):e0161988

S7883

BQ-123

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