1. GPCR/G Protein
  2. 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 (28):

Cat. No. Product Name Effect Purity
  • HY-15894
    BQ-788 sodium salt Antagonist 98.08%
    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-P0202
    Endothelin 1 swine, human Activator
    Endothelin 1 (swine, human) is a synthetic peptide with the Sequence: Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp (Disulfide bridge: Cys1-Cys15, Cys3-Cys11);CSCSSLMDKECVYFCHLDIIW (Disulfide bridge: Cys1-Cys15, Cys3-Cys11).
  • HY-14184
    Macitentan Antagonist 99.30%
    Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
  • 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-15403A
    Atrasentan hydrochloride Antagonist 99.66%
    Atrasentan (hydrochloride) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
  • HY-17351
    Tezosentan Antagonist
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
  • HY-12378
    BQ-123 Antagonist 98.39%
    BQ-123 is an ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively) .
  • 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-10088
    Zibotentan Antagonist 98.13%
    Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
  • HY-13209
    Ambrisentan Antagonist 99.86%
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
  • HY-15895
    Aprocitentan Antagonist
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.
  • HY-17621
    Sparsentan Antagonist 99.08%
    Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
  • HY-11103
    Sitaxsentan sodium Inhibitor 98.73%
    Sitaxsentan (sodium) is an orally active, highly selective antagonist of endothelin A receptors.
  • HY-16465
    IRL-1620 Agonist
    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM. Sequence: Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp;Suc-DEEAVYFAHLDIIW.
  • 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. Sequence: Ser-Leu-Arg-Arg-Ser-Ser-Cys-Phe-Gly-Gly-Arg-Ile-Asp-Arg-Ile-Gly-Ala-Gln-Ser-Gly-Leu-Gly-Cys-Asn-Ser-Phe-Arg-Tyr (Disulfide bridge: Cys7-Cys23);SLRRSSCFGGRIDRIGAQSGLGCNSFRY (Disulfide bridge: Cys7-Cys23).
  • HY-15403
    Atrasentan Antagonist
    Atrasentan is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
  • 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).
  • HY-15195
    Avosentan Antagonist 98.85%
    Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.
  • HY-B0323
    Sulfisoxazole Antagonist 99.96%
    Sulfisoxazole, an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent.
  • HY-106182
    Endothelin Mordulator 1 Modulator
    Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
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