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-14184R
    Macitentan (Standard)
    		Antagonist
    Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. 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).
    Macitentan (Standard)
  • HY-135283
    ABT-546
    		Antagonist
    ABT-546 (A-216546), a chemical probe, 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.
    (Rac)-Ambrisentan-d<sub>3</sub>
  • HY-105829S
    Sulfatroxazole-d4
    		Antagonist
    Sulfatroxazole-d4 (Isosulfafurazole-d4) is the deuterium labeled Sulfatroxazole (HY-105829). Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50 of 0.26 μM).
    Sulfatroxazole-d<sub>4</sub>
  • HY-P2496
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled
    		Agonist
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of ETA/ETB receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure.
    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-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 Antibody
    		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 Antibody
  • HY-A0013AR
    Bosentan hydrate (Standard)
    		Antagonist
    Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. 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.
    Bosentan hydrate (Standard)
  • HY-P10135
    RES-701-1
    		Antagonist
    RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ETB receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM.
    RES-701-1
  • HY-106337
    SB 247083
    		Antagonist
    SB 247083 is a selective, competitive and orally active endothelin-A receptor antagonist with a Ki of 0.41 nM. SB 247083 shows a Ki of 467 nM to endothelin-B receptor. SB 247083 shows a Kb of 3.5 nM for ET-1-induced contraction of rat aorta. SB 247083 can be used for the research of cardiovascular disease.
    SB 247083
  • HY-112264
    ETA antagonist 1
    		Antagonist
    ETA antagonist 1 is a ETA selective antagonist with an IC50 of 0.08 μM.
    ETA antagonist 1
  • HY-P1112A
    Sarafotoxin S6a TFA
    		Agonist
    Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM.
    Sarafotoxin S6a TFA
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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