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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Avosentan (Standard)
0 ImagesSynonyms: Ro 67-0565 (Standard); SPP-301 (Standard)Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan 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.
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IRL-3630
0 ImagesCat. No.: HY-118695CAS No.: 173189-01-0IRL-3630 (Compound 3) is an ETA/ETB antagonist (Ki: 1.9 and 1.2 nM).
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Nebentan potassium (Standard)
0 ImagesCat. No.: HY-106994ARCAS No.: 342005-82-7Synonyms: YM598 (Standard)Nebentan potassium (Standard) (GT-2331 maleate (Standard)) is the analytical standard of Nebentan (potassium) (HY-106994A). This product is intended for research and analytical applications. 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.
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Aminaftone
0 ImagesCat. No.: HY-19890CAS No.: 14748-94-8Synonyms: Aminaftone; AminaphthoneAminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
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PD-159020
0 ImagesCat. No.: HY-101598CAS No.: 177904-00-6PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.
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ZD-1611
0 ImagesCat. No.: HY-19274CAS No.: 186497-38-1ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
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Clazosentan disodium
0 ImagesSynonyms: Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodiumClazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction.
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Aprocitentan (Standard)
0 ImagesSynonyms: ACT-132577 (Standard)Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
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ETA antagonist 2
0 ImagesCat. No.: HY-78323CAS No.: 290815-30-4ETA antagonist 2 (Example 1) is an ETA antagonist.
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SB-209670
0 ImagesCat. No.: HY-19210CAS No.: 157659-79-5SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty.
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Aselacin A
0 ImagesCat. No.: HY-N5170CAS No.: 156223-06-2Aselacin A targets endothelin-1 receptor (ET-1 receptor), inhibits the the binding of ET-1 to ETA receptor and ETB receptor. Aselacin A inhibits the ET-1 binding to bovine atrial membrane and porcine cerebral membrane with IC50 of 22 μg/mL and 20 μg/mL. Aselacin A can be used for research of cardiovascular diseases.
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WS009A
0 ImagesCat. No.: HY-120843CAS No.: 136286-49-2WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases.
