Endothelin Receptor

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.