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 (17):

Cat. No. Product Name Effect Purity
  • HY-14184
    Macitentan Antagonist
    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
    Atrasentan (hydrochloride) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
  • HY-A0013
    Bosentan Antagonist
    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-15894
    BQ-788 sodium salt Antagonist
    BQ-788 (sodium salt) is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
  • HY-A0013A
    Bosentan hydrate Antagonist
    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-13209
    Ambrisentan Antagonist
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
  • HY-11103
    Sitaxsentan sodium Inhibitor
    Sitaxsentan (sodium) is an orally active, highly selective antagonist of endothelin A receptors.
  • HY-15195
    Avosentan Antagonist
    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, which is dual ETA/ETB antagonist designed for tissue targeting.
  • HY-12378
    BQ-123 Antagonist
    BQ-123 is an ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively) .
  • HY-10088
    Zibotentan Antagonist
    Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
  • 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. 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-76520
    sitaxsentan Antagonist
    Sitaxsentan (IPI 1040; TBC 11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.
  • HY-15894A
    BQ-788 Antagonist
    BQ-788 is a potent and selective endothelin receptor subtype B (ETB) antagonist with IC50 of 1.2 nM(inhibits 125I-labeled endothelin 1 (ET-1) binding to ETB receptors on human Girardi heart cells).