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-B0323
    Sulfisoxazole
    		Antagonist 99.90%
    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-10088
    Zibotentan
    		Antagonist 99.17%
    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
  • HY-17352
    Clazosentan
    		Antagonist 98.01%
    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
  • HY-16465A
    IRL-1620 TFA
    		Agonist 99.74%
    IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
    IRL-1620 TFA
  • HY-P0207A
    Endothelin-2 (49-69), human TFA
    		Ligand 98.78%
    Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
    Endothelin-2 (49-69), human TFA
  • HY-120295
    A-192621
    		Antagonist 99.85%
    A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
    A-192621
  • HY-15404
    Darusentan
    		Inhibitor 98.67%
    Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM.
    Darusentan
  • HY-P1237A
    C-Type Natriuretic Peptide (CNP) (1-22), human TFA
    		Agonist 98.10%
    C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor.
    C-Type Natriuretic Peptide (CNP) (1-22), human TFA
  • HY-17351
    Tezosentan
    		Antagonist 98.79%
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
    Tezosentan
  • HY-103460
    IRL 2500
    		Antagonist 99.27%
    IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50?values of 1.3 and 94 nM for ETB?and ETA?receptors, respectively. IRL 2500 inhibits ETB?receptor-mediated blood pressure increase and renal vascular resistance in rats?in vivo.
    IRL 2500
  • HY-15195
    Avosentan
    		Antagonist 98.15%
    Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.
    Avosentan
  • HY-118497
    BMS 182874
    		Antagonist 99.85%
    BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research.
    BMS 182874
  • HY-14184A
    Macitentan (n-butyl analogue)
    		99.35%
    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Macitentan (n-butyl analogue)
  • HY-102029
    Sarafotoxin S6c
    		Agonist 98.19%
    Sarafotoxin S6c (SRTX-c) is a potent endothelin-B receptor agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels.
    Sarafotoxin S6c
  • HY-P5792
    Atrial natriuretic peptide (3-28) (human)
    		99.65%
    Atrial natriuretic peptide (3-28) (human) (ANP (3-28) (human)) is a peptide hormone that is synthesized and secreted by the atrial myocardium. Atrial natriuretic peptide (3-28) (human) is involved in the regulation of blood pressure, fluid balance, and electrolyte homeostasis.
    Atrial natriuretic peptide (3-28) (human)
  • HY-106994A
    Nebentan potassium
    		Antagonist 99.53%
    Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
    Nebentan potassium
  • HY-19431
    Ro 46-8443
    		Antagonist 98.93%
    Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM).
    Ro 46-8443
  • HY-106994
    Nebentan
    		Antagonist 99.67%
    Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
    Nebentan
  • HY-121300
    Kendomycin
    		Antagonist 98.00%
    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-P0207
    Endothelin-2 (49-69), human
    		Ligand
    Endothelin-2 (49-69), human (Endothelin-2 (human, canine)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
    Endothelin-2 (49-69), human
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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