1. Signaling Pathways
  2. GPCR/G Protein
  3. Endothelin Receptor

Endothelin Receptor

Endothelin receptors are G protein-coupled receptors whose activation results in elevation of intracellular-free calcium. There are at least four type known, ETA, ETB1, ETB2 and ETC. ETA is a subtype for vasoconstriction. These receptors are found in the smooth muscle tissue of blood vessels, and binding of endothelin to ETA increases vasoconstriction (contraction of the blood vessel walls) and the retention of sodium, leading to increased blood pressure. ETB1 mediates vasodilation, when endothelin binds to ETB1 receptors, this leads to the release of nitric oxide (also called endothelium-derived relaxing factor), natriuresis and diuresis (the production and elimination of urine) and mechanisms that lower blood pressure. ETB2 mediates vasoconstriction. ETC has yet no clearly defined function. ET receptors are also found in the nervous system where they may mediate neurotransmission and vascular functions.

Endothelin Receptor Related Products (33):

Cat. No. Product Name Effect Purity
  • HY-P0202
    Endothelin 1 (swine, human) Activator
    Endothelin 1 (swine, human) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB.
  • HY-15894
    BQ-788 sodium salt Antagonist 98.03%
    BQ-788 (sodium salt) is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
  • HY-A0013
    Bosentan Antagonist 99.69%
    Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
  • HY-12378
    BQ-123 Antagonist
    BQ-123 is a selective endothelin A receptors (ETAR) antagonist with an IC50 value of 7.3 nM and a Ki vaule of 25 nM.
  • HY-14184
    Macitentan Antagonist 99.93%
    Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
  • HY-15404
    Darusentan Inhibitor 98.66%
    Darusentan is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM.
  • HY-16465A
    IRL-1620 TFA Agonist
    IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
  • HY-P1016A
    BQ-3020 TFA Agonist
    BQ-3020 (TFA) is a selective agonist of ETB receptor, inhibits [125I]ET-1 binding to ETB receptor with an IC50 of 0.2 nM in cerebellum, and causes vasoconstriction.
  • HY-A0013A
    Bosentan (hydrate) Antagonist 99.94%
    Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
  • HY-15403A
    Atrasentan hydrochloride Antagonist 99.80%
    Atrasentan hydrochloride (ABT-627 hydrochloride) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
  • HY-13209
    Ambrisentan Antagonist 99.86%
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
  • HY-17621
    Sparsentan Antagonist 99.08%
    Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
  • HY-P1235A
    Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate Inhibitor 99.27%
    Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. ANP (1-28) inhibits endothelin-1 secretion in a dose-dependent way.
  • HY-B0323
    Sulfisoxazole Antagonist 99.96%
    Sulfisoxazole, an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent.
  • HY-10088
    Zibotentan Antagonist 99.66%
    Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
  • HY-P1236
    Atrial Natriuretic Peptide (ANP) (1-28), rat Inhibitor
    Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-15895
    Aprocitentan Antagonist 98.13%
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.
  • HY-11103
    Sitaxsentan sodium Inhibitor 98.73%
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.
  • HY-15195
    Avosentan Antagonist 98.36%
    Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.
  • HY-14184A
    Macitentan (n-butyl analogue)
    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
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