Endothelin Receptor
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
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Endothelin Receptor Inhibitors
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Endothelin Receptor Agonists
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Endothelin Receptor Antagonists
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Endothelin Receptor Activators
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Endothelin Receptor Modulator
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Endothelin Receptor Control
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Endothelin Receptor Ligands
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Endothelin Receptor Proteins
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Endothelin Receptor Type A (EDNRA) Proteins
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Endothelin R Type B (EDNRB) Proteins
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Endothelin Receptor Related Products (152)
Related Products (152)
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Recombinant Proteins (7)
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Antibodies (1)
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Endothelin Receptor Isoform Comparison
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PD 155080
0 ImagesCat. No.: HY-105362CAS No.: 162412-71-7PD 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.
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Sulfatroxazole
0 ImagesCat. No.: HY-105829CAS No.: 23256-23-7Synonyms: IsosulfafurazoleSulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50=0.26 μM).
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BE 24566B
0 ImagesCat. No.: HY-W781265CAS No.: 149466-04-6Synonyms: L-755,805BE 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).
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Sparsentan-d5
0 ImagesCat. No.: HY-17621SCAS No.: 1801597-09-0Synonyms: RE-021-d5; DARA-a-d5Sparsentan-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.
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Daglutril
0 ImagesCat. No.: HY-10282CAS No.: 182821-27-8Daglutril 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.
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PD 156252
0 ImagesCat. No.: HY-P10151CAS No.: 175592-65-1PD 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.
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BQ-610
0 ImagesCat. No.: HY-135446CAS No.: 141595-53-1BQ-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.
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ABT-546 hydrochloride
0 ImagesCat. No.: HY-19309CAS No.: 223756-43-2Synonyms: A-216546 hydrochlorideABT-546 (A-216546) hydrochloride is an orally active ETA receptor antagonist, with Ki values of 0.46 nM and 13000 nM for human ETA and ETB receptors, respectively, and exhibits >25000-fold selectivity over the ETB receptor. ABT-546 hydrochloride effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC50 = 0.59 nM) and arachidonic acid release (IC50 = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 hydrochloride crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 hydrochloride inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 hydrochloride can be used for research on abdominal aortic aneurysm.
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[Ala2] Endothelin-3, human
![[Ala2] Endothelin-3, human](https://file.medchemexpress.com/product_pic/hy-p3571.gif "Click to View [Ala2] Endothelin-3, human Product Detail")
0 ImagesCat. No.: HY-P3571CAS No.: 2243207-08-9[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.
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ACT-373898
0 ImagesCat. No.: HY-135500CAS No.: 1433875-14-9ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist.
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TA-0201
0 ImagesCat. No.: HY-124234CAS No.: 169679-53-2TA-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.
![[Ala18] Endothelin-1, human](https://file.medchemexpress.com/product_pic/hy-p3610.gif "Click to View [Ala18] Endothelin-1, human Product Detail")
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ANP (1-30), frog
0 ImagesCat. No.: HY-P3762CAS No.: 309245-16-7ANP (1-30), frog is a peptide fragment of atrial natriuretic peptide derived from frog. ANP (1-30), frog has natriuretic, diuretic, and vasorelaxant effects.
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PD 145065
0 ImagesCat. No.: HY-105183CAS No.: 153049-49-1PD 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.
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SB234551
0 ImagesCat. No.: HY-101262CAS No.: 188257-69-4SB234551 is a selective endothelin ETA receptor antagonist. SB234551 can be used in the study of stroke model.
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Endothelin (16-21)
0 ImagesCat. No.: HY-P5769CAS No.: 121377-67-1Endothelin (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.
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Big Endothelin-1 (22-38), human
0 ImagesCat. No.: HY-P3733CAS No.: 124932-61-2Big 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).
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SM19712 free acid
0 ImagesCat. No.: HY-120148CAS No.: 194542-49-9SM19712 free acid is an orally active, selective endothelin converting enzyme (ECE) inhibitor. SM19712 free acid inhibits conversion of big ET-1 to ET-1. SM19712 free acid attenuates colonic angiogenesis, tissue injury, inflammation, without altering colon shortening or myeloperoxidase levels in mice. SM19712 free acid can be used for the research of inflammatory bowel disease (colitis), ischemic acute renal failure, acute myocardial infarction, and myocardial ischemia/reperfusion injury.
