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 (23):

Cat. No. Product Name Effect Purity
  • HY-14184
    Macitentan Antagonist 99.95%
    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-15403A
    Atrasentan hydrochloride Antagonist 99.66%
    Atrasentan (hydrochloride) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
  • HY-15894
    BQ-788 sodium salt Antagonist 98.08%
    BQ-788 sodium salt is a potent, selective ETB receptor antagonist (IC50 = 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells); poorly inhibited the binding to ET A receptors in human neuroblastoma cell line SK-N-MC cells (IC(50), 1300 nM).
  • HY-A0013
    Bosentan Antagonist 99.67%
    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-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-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.
  • 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-16465
    IRL-1620 Agonist
    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
  • HY-13209
    Ambrisentan Antagonist 99.86%
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
  • 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-15195
    Avosentan Antagonist 98.85%
    Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.
  • HY-15895
    ACT-132577 Antagonist
    ACT-132577 is the major and pharmacologically active metabolite of macitentan(ACT-064992), which is dual ETA/ETB endothelin (ET) receptor antagonist designed for tissue targeting.
  • 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-11103
    Sitaxsentan sodium Inhibitor 98.06%
    Sitaxsentan sodium (IPI 1040; TBC 11251) is a selective endothelin A (ETA) receptor antagonist.
  • HY-B0323
    Sulfisoxazole Antagonist
    Sulfisoxazole, an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent.
  • HY-15403
    Atrasentan Antagonist
    Atrasentan (A-147627; ABT 627) is an endothelin receptor antagonist (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.
  • HY-19529
    Ro 46-2005 Antagonist
    Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.
  • HY-14184A
    Macitentan n-butyl analogue
    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan.
  • HY-19890
    Aminaftone Inhibitor
    Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
  • HY-101598
    PD-159020 Antagonist
    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.