2. Signaling Pathways
  3. GPCR/G Protein
  4. Endothelin Receptor

Endothelin Receptor

Endothelin Receptor

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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 Isoform Specific Products:

Endothelin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16465
    IRL-1620
    		Agonist
    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
    IRL-1620
  • HY-P1235
    Carperitide
    		Inhibitor
    Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
    Carperitide
  • HY-P1236A
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA
    		Inhibitor
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA
  • HY-14184S
    Macitentan-d4
    		Antagonist 98.03%
    Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan 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].
    Macitentan-d<sub>4</sub>
  • HY-15895S
    Aprocitentan-d4
    		Antagonist
    Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a 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.
    Aprocitentan-d<sub>4</sub>
  • HY-19529
    Ro 46-2005
    		Antagonist 98.32%
    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.
    Ro 46-2005
  • HY-135283
    ABT-546
    		Antagonist
    ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
    ABT-546
  • HY-12378A
    BQ-123 TFA
    		Antagonist
    BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
    BQ-123 TFA
  • HY-13209C
    Ambrisentan sodium
    		Antagonist
    Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist.
    Ambrisentan sodium
  • HY-115417
    Bosentan-d4
    		Antagonist
    Bosentan-d4 is the deuterium labeled Bosentan. 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.
    Bosentan-d4
  • HY-13209BS
    (Rac)-Ambrisentan-d3
    (Rac)-Ambrisentan-d3 is the deuterium labeled (Rac)-Ambrisentan[1].
    (Rac)-Ambrisentan-d<sub>3</sub>
  • 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.
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled
  • 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
    [Ala1,3,11,15]-Endothelin (53-63)
  • 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.
    BMS-193884
  • 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.
    BMS-248360
  • HY-119667
    Enrasentan
    		Antagonist
    Enrasentan (SB 217242) is an endothelin (ET) receptor antagonist. Enrasentan has antihypertensive effects.
    Enrasentan
  • 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.
    Methylsolfonyl 25(S)-Δ7-dafachronic acid
  • HY-106182
    TBC3711
    		Modulator
    TBC3711 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
    TBC3711
  • HY-P3563
    [Lys4] Sarafotoxin S6c
    		Agonist
    [Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC50 of 1.5 nM.
    [Lys4] Sarafotoxin S6c
  • HY-P990573
    DEDN6526A (RG-7636)
    		Inhibitor
    DEDN6526A (RG-7636) is a humanized antibody expressed in CHO cells, targeting ETBR. DEDN6526A (RG-7636) has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for DEDN6526A (RG-7636) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    DEDN6526A (RG-7636)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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