Endothelin Receptor

Choose Selective Endothelin Receptor Inhibitors

Endothelin Receptor Signaling Pathway Map

Endothelin Receptor Signaling Pathways
Isoform-selective Inhibitors

Endothelin Receptor Products

  • All (6)
  • Endothelin Receptor Antagonists (6)
  • New Endothelin Receptor Products
Catalog No. Product Name 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.
Hepatology, 2016, 63(3):1000-12
Oncotarget, 2016, 7(47):77138-77151
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).
Eur J Pharmacol, 2019, 855:124-136
Pharmacol Res Perspect, 2017, 5(6)
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.
Cardiovasc Res, 2021, 117(5):1391-1401
Wiley Online Library, 2021, 10.1002/adtp.202000289
J Pers Med, 2021, 11(6)509
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.
Biomedicines, 2021, 10(1)86
S7883 BQ-123 BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12764
Biomed Res Int, 2019, 2019:3851718
ZANCO, 2019, 31-2
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.
Biomedicines, 2022, 10(3)629
Front Pharmacol, 2021, 12:740529
Front Med (Lausanne), 2021, 8:742436
S1456 Zibotentan (ZD4054) Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.
Hepatology, 2016, 63(3):1000-12
Oncotarget, 2016, 7(47):77138-77151
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).
Eur J Pharmacol, 2019, 855:124-136
Pharmacol Res Perspect, 2017, 5(6)
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.
Cardiovasc Res, 2021, 117(5):1391-1401
Wiley Online Library, 2021, 10.1002/adtp.202000289
J Pers Med, 2021, 11(6)509
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.
Biomedicines, 2021, 10(1)86
S7883 BQ-123 BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12764
Biomed Res Int, 2019, 2019:3851718
ZANCO, 2019, 31-2
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.
Biomedicines, 2022, 10(3)629
Front Pharmacol, 2021, 12:740529
Front Med (Lausanne), 2021, 8:742436