Home GPCR & G Protein Endothelin Receptor

Endothelin Receptor antagonists

ETA Receptor which is a G-protein-coupled receptor for ETs which are three small peptides: ET-1, ET-2 and ET3. ET-1 activates various kinases that are known to be involved in the survival of cell signalling and proliferation, including protein kinase C (PKC), epidermal growth factor (EGF), insulin-like growth factor-1 and mitogen-activated protein kinase (MAPK). ETA Receptor also contributes to induction of the early-response genes c-FOS, c-JUN and c-MYC. The downstream mediators of ETA-receptor include SHC, GRB2, p38 and ERK. ET-1 acting through ETA can inhibits paclitaxel-induced apoptosis by triggering anti-apoptotic signalling through BCL2-dependent and phosphatidylinositol 3-kinase-mediated Akt pathways.

Other GPCR & G Protein Related Inhibitors

Hedgehog/Smoothened PKA CGRP Receptor S1P Receptor Cannabinoid Receptor SGLT Opioid Receptor GPR CCR MT Receptor

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
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.
J Immunother Cancer, 2024, 12(11)e009805
Transl Oncol, 2024, 44:101944
Ann Dermatol, 2024, 36(3):151-162
S8051 Macitentan Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.
Nat Cancer, 2025, 10.1038/s43018-025-00963-w
J Immunother Cancer, 2024, 12(11)e009805
Biosci Rep, 2024, 44(12)BSR20241320
S7883 BQ-123 BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
Nat Biomed Eng, 2025, 10.1038/s41551-025-01419-3
Redox Biol, 2025, 80:103493
Am J Physiol Heart Circ Physiol, 2025, 328(3):H484-H495
Verified customer review of BQ-123
S1456 Zibotentan (ZD4054) Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. This compound is in Phase 3.
Cell Death Dis, 2023, 14(1):5
Hepatology, 2016, 63(3):1000-12
Oncotarget, 2016, 7(47):77138-77151
Verified customer review of Zibotentan (ZD4054)
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)
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.
Oncotarget, 2016, 7(20):29187-98
PLoS One, 2016, 11(9):e0161988
Verified customer review of Bosentan
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.
Front Pharmacol, 2022, 13:964370
Biomedicines, 2021, 10(1)86
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.
E3868 Pearl Extract Pearl Extract is extracted from pearl, which inhibits endothelin, thereby safely and effectively lightening the skin by antagonising endothelin.
E7301 Atrasentan Atrasentan (ABT-627, (+)-A 127722, A-147627) is an antagonist of endothelin A (ETA) receptor with a Ki of 0.034 nM. It exhibits antitumor activity by inhibiting prostate cancer cell growth and inducing apoptotic cell death.

Signaling Pathway Map