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-17352
    Clazosentan
    		Antagonist 99.50%
    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-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 99.37%
    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-P1237A
    C-Type Natriuretic Peptide (CNP) (1-22), human TFA
    		Agonist 99.07%
    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-16465A
    IRL-1620 TFA
    		Agonist 98.73%
    IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
    IRL-1620 TFA
  • HY-114367
    Delphinidin 3-rutinoside chloride
    		Activator 98.83%
    Delphinidin 3-rutinoside chloride is an anthocyanin component. Delphinidin 3-rutinoside chloride is isolable from the fruits of blackcurrant Ribes nigrum L. Delphinidin 3-rutinoside chloride activates the ETB receptor and stimulates the NO/cGMP pathway. Delphinidin 3-rutinoside chloride increases cyclic guanosine monophosphate production and reduces the phosphorylation level of Myosin regulatory light chain. Delphinidin 3-rutinoside chloride stimulates GLP-1 secretion. It significantly induces relaxation of bovine ciliary muscle strips contracted by ET-1 and inhibits ET-1-induced contraction of bovine ciliary muscle strips. Delphinidin 3-rutinoside chloride is applicable to research related to type 2 diabetes.
    Delphinidin 3-rutinoside chloride
  • HY-16465
    IRL-1620
    		Agonist 99.69%
    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
    IRL-1620
  • HY-P5792
    Atrial natriuretic peptide (3-28) (human)
    		99.86%
    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-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-17351
    Tezosentan
    		Antagonist 98.27%
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
    Tezosentan
  • HY-W042301
    Xipamide
    		Control 99.74%
    Xipamide is an orally active carbonic anhydrase (CA) inhibitor and Na+/Cl--potassium transporter inhibitor with diuretic and antihypertensive effects. Xipamide reduces NaCl reabsorption by inhibiting the Cl-/NaCO3- anion exchanger, and increases calcium reabsorption while promoting potassium and magnesium excretion. Xipamide is mainly cleared via the renal pathway and causes a temporary decrease in glomerular filtration rate under specific conditions. Xipamide does not affect Ca2+ signaling induced by endothelin-1 and other factors, nor does it inhibit various ion cotransport or pump activities in red blood cells. Xipamide can be used in researches related to cardiovascular diseases, hypertension (especially with left ventricular hypertrophy), advanced renal failure, and liver cirrhosis with ascites.
    Xipamide
  • HY-P0207A
    Endothelin-2 (49-69), human TFA
    		Ligand 99.21%
    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-15404
    Darusentan
    		Inhibitor 98.60%
    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-P0204
    Endothelin-3, human, mouse, rabbit, rat
    Endothelin-3, human, mouse, rabbit, rat (Endothelin 3 (Rat,Human)) is an adhesion stimulant. Endothelin-3, human, mouse, rabbit, rat stimulates the adhesion of enteric neural crest cells to various ECM components. Endothelin-3, human, mouse, rabbit, rat plays an important role in the maintenance and self-renewal of intestinal progenitor cells, participates in the migration of enteric neural crest cells, and helps maintain a suitable environment for the colonization of enteric neural crest cells. Endothelin-3, human, mouse, rabbit, rat acts synergistically with the β1-integrin signaling pathway during enteric nervous system development. Endothelin-3, human, mouse, rabbit, rat can be used in studies related to distal aganglionosis.
    Endothelin-3, human, mouse, rabbit, rat
  • HY-120295
    A-192621
    		Antagonist 99.92%
    A-192621, a chemical probe, 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-N7543
    Schisantherin D
    		Inhibitor 99.66%
    Schisantherin D is a lignan. Schisantherin D can be isolated from Kadsura interior. Schisantherin D downregulates the expression of ETBR and inhibits the secretion of ECM and ET-1. Schisantherin D alleviates EtOH + ET-1-induced hepatocyte cytotoxicity. Schisantherin D potently inhibits HIV replication in cells.
    Schisantherin D
  • HY-15195
    Avosentan
    		Antagonist 98.15%
    Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure.
    Avosentan
  • HY-15895S
    Aprocitentan-d4
    		Antagonist 98.76%
    Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent.
    Aprocitentan-d<sub>4</sub>
  • HY-P1236A
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA
    		Inhibitor 99.32%
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) 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, mouse TFA
  • HY-P1112
    Sarafotoxin S6a
    		Agonist 98.59%
    Sarafotoxin S6a, 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 elicits the pig coronary artery with an EC50 value of 7.5 nM.
    Sarafotoxin S6a
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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