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-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-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-15402D
    Edonentan hydrate
    		Antagonist
    Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility.
    Edonentan hydrate
  • 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-123744
    PD-156707
    		Antagonist 99.92%
    PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist.
    PD-156707
  • HY-P2057
    PD 142893
    		Antagonist
    PD 142893 is a endothelin-B receptor antagonist.
    PD 142893
  • 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-P1419A
    AP 811 acetate
    		Antagonist
    AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation.
    AP 811 acetate
  • HY-P990089
    Patecibart
    		Antagonist
    Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an endothelin receptor antagonist.
    Patecibart
  • HY-P5130
    Big endothelin-1 (rat 1-39)
    		Ligand
    Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice.
    Big endothelin-1 (rat 1-39)
  • 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
  • HY-W781265
    BE 24566B
    		Antagonist
    BE 24566B is a polyketide fungal metabolite originally isolated from S. violaceusniger. It is active against B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus (MICs=1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/mL, respectively). BE 24566B is an endothelin (ET) receptor antagonist (IC50s=11 and 3.9 μM for ETA and ETB receptors, respectively).
    BE 24566B
  • HY-17621S
    Sparsentan-d5
    		Antagonist
    Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
    Sparsentan-d<sub>5</sub>
  • HY-10282
    Daglutril
    Daglutril is a compound with the potential to regulate cytokine-induced endothelin-1 production in astrocytes. In studies, it has an inhibitory effect on the production of endothelin-1 induced by some cytokines and can be used as a tool to screen compounds that inhibit endothelin-1 production in astrocytes.
    Daglutril
  • HY-105168
    TAK 044
    		Antagonist
    TAK 044 is an antagonist of Endothelin Receptor. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage.
    TAK 044
  • HY-P1019A
    [Ala1,​3,​11,​15]​-​Endothelin (53-63) (TFA)
    		Agonist
    [Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ETB with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction.
    [Ala1,​3,​11,​15]​-​Endothelin (53-63) (TFA)
  • HY-P10151
    PD 156252
    		Antagonist
    PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.
    PD 156252
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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