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-P0202
    Endothelin 1 (swine, human)
    		Activator 99.12%
    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)
  • HY-A0013
    Bosentan
    		Antagonist 99.98%
    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
  • HY-14184
    Macitentan
    		Antagonist 99.95%
    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
  • HY-P0202A
    Endothelin 1 (swine, human) (TFA)
    		99.95%
    Endothelin 1 (swine, human) (TFA) 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) (TFA)
  • HY-13209
    Ambrisentan
    		Antagonist 99.95%
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
    Ambrisentan
  • 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-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-P2057
    PD 142893
    		Antagonist
    PD 142893 is a endothelin-B receptor antagonist.
    PD 142893
  • HY-15894A
    BQ-788
    		Antagonist 98.66%
    BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
    BQ-788
  • HY-15403A
    Atrasentan hydrochloride
    		Antagonist 99.82%
    Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA.
    Atrasentan hydrochloride
  • HY-12378
    BQ-123
    		Antagonist 99.78%
    BQ-123 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 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
    BQ-123
  • HY-A0013A
    Bosentan (hydrate)
    		Antagonist 99.85%
    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)
  • HY-15894
    BQ-788 sodium salt
    		Antagonist 98.56%
    BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
    BQ-788 sodium salt
  • HY-P1235A
    Carperitide acetate
    		Inhibitor 99.15%
    Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way.
    Carperitide acetate
  • HY-P0204A
    Endothelin-3, human, mouse, rabbit, rat TFA
    		99.51%
    Endothelin-3, human, mouse, rabbit, rat TFA is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
    Endothelin-3, human, mouse, rabbit, rat TFA
  • HY-B0323
    Sulfisoxazole
    		Antagonist 99.95%
    Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
    Sulfisoxazole
  • HY-P1236
    Atrial Natriuretic Peptide (ANP) (1-28), rat
    		Inhibitor
    Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
    Atrial Natriuretic Peptide (ANP) (1-28), rat
  • HY-11103
    Sitaxsentan sodium
    		Inhibitor 99.03%
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.
    Sitaxsentan sodium
  • HY-17621
    Sparsentan
    		Antagonist 99.17%
    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
  • HY-10088
    Zibotentan
    		Antagonist 98.19%
    Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
    Zibotentan
Cat. No. Product Name / Synonyms Species Source