2. GPCR/G Protein
  3. Endothelin Receptor

Endothelin Receptor

Endothelin receptors are G protein-coupled receptors (GPCRs) of the β-group of rhodopsin receptors that bind to endothelin ligands, which are 21 amino acid long peptides derived from longer prepro-endothelin precursors. There are at least four types known, ETA, ETB (ETB1, ETB2) and ETC. The ETA receptor is characterized by having high affinity and selectivity for ET-1 and ET-2 compared to ET-3, whereas the ETB receptor has equivalent high affinity for all three endothelin isopeptides.

Endothelins are synthesized in several tissues, including the vascular endothelium (ET-1 exclusively) and smooth muscle cells. Released endothelin binds to the endothelin receptors ETA and ETB, the ETA receptors on vascular smooth muscle cells mediating vasoconstriction, and the ETB receptors on the endothelium linked to nitric oxide (NO) and prostacyclin release.

Endothelin Receptor Related Products (116):

Cat. No. Product Name Effect Purity
  • HY-14184
    Macitentan Antagonist
    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)[1].
  • HY-P0202
    Endothelin 1 (swine, human) Activator 99.12%
    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[1].
  • HY-13209
    Ambrisentan Antagonist 99.95%
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
  • HY-A0013
    Bosentan Antagonist 99.98%
    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-P0204A
    Endothelin-3, human, mouse, rabbit, rat TFA 99.96%
    Endothelin-3, human, mouse, rabbit, rat TFA is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
  • HY-105829S
    Sulfatroxazole-d4 Antagonist
    Sulfatroxazole-d4 (Isosulfafurazole-d4) is the deuterium labeled Sulfatroxazole (HY-105829)[1]. Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50 of 0.26 μM)[2].
  • HY-10088R
    Zibotentan (Standard) Antagonist
    Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research[1][2].
  • HY-76520S
    Sitaxsentan-13C6 Antagonist
    Sitaxsentan-13C6 (IPI 1040-13C6) is 13C labeled Sitaxsentan.
  • HY-15403
    Atrasentan Antagonist 99.58%
    Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA[1].
  • 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[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2].
  • 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[1].
  • HY-126036
    CH-141 Antagonist
    CH-141 is a peripheral vasodilator, that can be used in hypertension research[1].
  • HY-P1019
    [Ala1,3,11,15]-Endothelin (53-63) Agonist
    [Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ETB with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction[1]
  • HY-15895
    Aprocitentan Antagonist 99.98%
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent[1].
  • HY-19263
    BMS-193884 Antagonist
    BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor[1].
  • HY-114953
    BMS-248360 Antagonist
    BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects[1].
  • HY-119667
    Enrasentan Antagonist
    Enrasentan (SB 217242) is an endothelin (ET) receptor antagonist. Enrasentan has antihypertensive effects[1].
  • 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[1][2][3].
  • HY-157940
    Methylsolfonyl 25(S)-Δ7-dafachronic acid Agonist
    Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with the IC50 of 0.41 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid shows low cell cytotoxicity in HepG2 cells with IC50 of >200 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid can be used for study of parasitism[1].
  • HY-15404
    Darusentan Inhibitor 98.67%
    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[1]. 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[2].