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 (40):

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-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-106994
    Nebentan free base Antagonist
    Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
  • HY-120295
    A-192621 Antagonist
    A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
  • HY-135283
    ABT-546 Antagonist
    ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
  • HY-14184
    Macitentan Antagonist 99.87%
    Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  • HY-15403A
    Atrasentan hydrochloride Antagonist 99.80%
    Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA.
  • 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-13209
    Ambrisentan Antagonist 99.86%
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
  • 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-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. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
  • 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-15195
    Avosentan Antagonist 98.36%
    Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.
  • 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-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.
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