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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-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-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-121300
    Kendomycin
    		Antagonist
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
    Kendomycin
  • HY-P1016B
    BQ-3020 ammonium
    		Agonist 99.18%
    BQ-3020 ammonium is a selective endothelin receptor (ETB receptor) agonist. BQ-3020 ammonium inhibits [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research. .
    BQ-3020 ammonium
  • 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
  • HY-B0323A
    Sulfisoxazole diethanolamine
    		Antagonist
    Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A.
    Sulfisoxazole diethanolamine
  • 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-123744
    PD-156707
    		Antagonist
    PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist.
    PD-156707
  • HY-P3433
    Sarafotoxin S6b
    		Agonist
    Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively.
    Sarafotoxin S6b
  • HY-103459
    CI-1020
    		Antagonist
    CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration.
    CI-1020
  • HY-P990089
    Patecibart
    		Antagonist
    Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an endothelin receptor antagonist.
    Patecibart
  • HY-P1016
    BQ-3020
    		Antagonist
    BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.
    BQ-3020
Cat. No. Product Name / Synonyms Species Source