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-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-P3228
    JKC 302
    		Antagonist
    JKC 302 is an ET-A receptor antagonist. JKC 302 partly blocks ET-1-induced contraction in asthmatic rat trachea ring.
    JKC 302
  • HY-P2057
    PD 142893
    		Antagonist
    PD 142893 is a endothelin-B receptor antagonist.
    PD 142893
  • HY-157658
    K-8794
    		Antagonist
    K-8794 is an orally active selective endothelin receptor ETB antagonist that can be used in research on cardiovascular diseases.
    K-8794
  • HY-P11605
    Big endothelin-3 (Human, 1-41 amide)
    Big endothelin-3 (Human, 1-41 amide) is a precursor molecule of the Endothelin-3 (ET-3) peptide composing of 41 amino acids.
    Big endothelin-3 (Human, 1-41 amide)
  • HY-13711
    S-1255
    		Inhibitor
    S-1255 is an orally active and highly selective endothelin ETA receptor antagonist (Kd=0.39 nM). S-1255 blocks vasoconstriction and sustains hypotensive effects in hypertensive rats. S-1255 is promising for research of hypertension and cardiovascular disorders.
    S-1255
  • HY-117814
    BMS-187308
    		Antagonist
    BMS-187308 is an orally active endothelin-A (ETA) antagonist, with Kis of 4.7 nM for ETA and 1.7 μM for ETB. BMS-187308 inhibits the pressor response to ET-1 (ED25: 1.2 µmol/kg; iv). BMS-187308 is a suitable tool for investigating the role of endothelin.
    BMS-187308
  • 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-182561
    Cgs 27830
    		Antagonist
    Cgs 27830 is an endothelin receptor antagonist with 20-fold higher selectivity for ET-A receptors over ET-B receptors. Cgs 27830 blocks activity of ET-A and ET-B receptors. Cgs 27830 does not alter basal vascular tone in the ovine fetal pulmonary circulation. Cgs 27830 prevents big-endothelin-1-induced pulmonary vasoconstriction in late gestation fetal lambs.
    Cgs 27830
  • 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-105408A
    Fandosentan potassium
    		Antagonist
    Fandosentan potassium is a potent endothelin A receptor (ETAR) antagonist. Fandosentan potassium inhibits CYP2C9 and CYP3A4 activities with IC50 values of 39.6 and 21.6 μM, respectively. Fandosentan potassium reverses the hypoxic pulmonary vasoconstriction in the perinatal lamb. Fandosentan potassium can be used for pulmonary hypertension research[1][2].
    Fandosentan potassium
  • 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-105362
    PD 155080
    		Inhibitor
    PD 155080 is a selective endothelin A receptor (ETA receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases.
    PD 155080
  • HY-105829
    Sulfatroxazole
    		Antagonist
    Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50=0.26 μM).
    Sulfatroxazole
  • 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.
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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