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-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-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
  • HY-135446
    BQ-610
    		Antagonist
    BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders.
    BQ-610
  • HY-171734
    DEDN6526A
    		Antagonist
    DEDN6526A is an antibody-drug conjugate (ADC) consisting of the humanized anti-ETBR antibody DEDN6526A (RG-7636) (HY-P990573 conjugated with valine-citrulline (vc) and the tubulin inhibitor MMAE (McMMAF) (HY-15575). DEDN6526A induces apoptosis and can be used in melanoma research.
    DEDN6526A
  • HY-P3571
    [Ala2] Endothelin-3, human
    [Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) where substitution of Ala for Cys residues. TE-3 is a vasoactive peptide, produced by human rhabdomyosarcoma cell lines, whereas it is not expressed by human sarcoma cell lines of non-muscle origin. ET-3 acts as a paracrine factor, since it promotes migration of endothelial cells.
    [Ala2] Endothelin-3, human
  • HY-135500
    ACT-373898
    ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist.
    ACT-373898
  • HY-124234
    TA-0201
    		Antagonist
    TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1.
    TA-0201
  • HY-P3610
    [Ala18] Endothelin-1, human
    [Ala18] Endothelin-1, human is a biologically active peptide. [Ala18] Endothelin-1, human can be used for the research of various biochemical studies.
    [Ala18] Endothelin-1, human
  • HY-P3762
    ANP (1-30), frog
    ANP (1-30), frog is a peptide fragment of atrial natriuretic peptide derived from frog. ANP (1-30), frog has natriuretic, diuretic, and vasorelaxant effects.
    ANP (1-30), frog
  • HY-105183
    PD 145065
    		Antagonist
    PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells.
    PD 145065
  • HY-101262
    SB234551
    		Antagonist
    SB234551 is a selective endothelin ETA receptor antagonist. SB234551 can be used in the study of stroke model.
    SB234551
  • HY-P5769
    Endothelin (16-21)
    		Agonist
    Endothelin (16-21) is a selective ETB receptor agonist (EC50=228 nM in guinea-pig bronchus). Endothelin (16-21) can induce smooth muscle contraction. Endothelin (16-21) is promising for research of respiratory (e.g., asthma) and cardiovascular (e.g., hypertension) diseases.
    Endothelin (16-21)
  • HY-P3733
    Big Endothelin-1 (22-38), human
    Big Endothelin-1 (22-38), human is derived from human, is the 22-38 fragment of Big Endothelin-1 (ET-1) (1-38). Big ET-1 (1-38) is a propeptide of ET-1, which has potent and long-lasting vasoconstrictor effects, equips a specific enzymatic cleavage of the 38 amino acid chain to form ET-1 (1-21) and the C-terminal fragment Big ET-1 (22-38).
    Big Endothelin-1 (22-38), human
  • HY-P3615
    [Asn18] Endothelin-1 (swine, human)
    		Agonist
    [Asn18] Endothelin-1 swine, human is a structural analogue of Endothelin 1 (swine, human) (HY-P0202), with the Asp amino acid at position 18 mutated to Asn. Endothelin 1 (swine, human) is a synthetic peptide with human and porcine endothelin 1 sequences and is a potent endogenous vasoconstrictor.
    [Asn18] Endothelin-1 (swine, human)
  • HY-17352R
    Clazosentan (Standard)
    		Antagonist
    Clazosentan (Standard) is the analytical standard of Clazosentan. This product is intended for research and analytical applications. Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction.
    Clazosentan (Standard)
  • HY-126036
    CH-141
    		Antagonist
    CH-141 is a peripheral vasodilator, that can be used in hypertension research.
    CH-141
  • HY-13209R
    Ambrisentan (Standard)
    		Antagonist
    Ambrisentan (Standard) is the analytical standard of Ambrisentan. This product is intended for research and analytical applications. Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
    Ambrisentan (Standard)
  • HY-76520
    Sitaxsentan
    		Antagonist
    Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
    Sitaxsentan
  • HY-114674
    A-127722
    		Inhibitor
    A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ETA selective endothelin receptor (ET receptor) antagonist with IC50 value of 0.36 nM.
    A-127722
  • HY-117644
    L-749329
    		Antagonist
    L-749329 ((Rac)-L-754142) is an ETA and ETB receptor antagonist, with Kis of 0.062 nM and 2.25 nM for ETA and ETB respectively. L-749329 inhibits ET-1-stimulated signaling.
    L-749329
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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