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 (42):

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 99.93%
    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 99.87%
    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-106994
    Nebentan Antagonist 99.67%
    Nebentan (YM598 free base) 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-P2496
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled Activator
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic Endothelin 1 peptide labled with Alexa Fluor 488. 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-121300
    Kendomycin Antagonist
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
  • HY-A0013A
    Bosentan (hydrate) Antagonist 99.71%
    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-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-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-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 (Sulfafurazole), an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
  • 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 (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM.
Isoform Specific Products

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.