Endothelin ligands, which are 21 amino acid long peptides derived from longer prepro-endothelin precursors, bind to endothelin receptors, G protein-coupled receptors (GPCRs) of the -group of rhodopsin receptors. At least four types are recognized: ETA, ETB (ETB1, ETB2), and ETC. The ETB receptor has an equivalently high affinity for all three endothelin isopeptides, whereas the ETA receptor exhibits high affinity and selectivity for ET-1 and ET-2 over ET-3.
Vascular endothelium (ET-1 exclusively) and smooth muscle cells are two tissues that produce endothelins. Endothelin receptors ETA and ETB, found on vascular smooth muscle cells that mediate vasoconstriction and the endothelium that is associated with the release of nitric oxide (NO) and prostacyclin, respectively, bind to released endothelin.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V33704 | Endothelin 1 swine, human | 117399-94-7 | Endothelin 1 (swine, human), a synthetic 21 amino acid peptide with the sequence of human and swine Endothelin 1 with potent vasoconstrictive action, is a potent endogenous vasoconstrictor. |
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V77038 | Endothelin-3, human, mouse, rabbit, rat TFA (Endothelin 3 (Rat,Human) (TFA)) | Endothelin-3, human, mouse, rabbit, rat TFA is a vasoactive peptide consisting of 21 amino acid (AA)s that binds to G protein-linked transmembrane receptors, ET-RA and ET-RB. | |
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V76879 | IRL-1620 TFA | IRL-1620 (TFA) is a potent and specific endorphin receptor (endothelin receptor) type B agonist/activator with a Ki of 16 pM. | |
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V1510 | Macitentan (ACT-064992 D4) | 441798-33-0 | Macitentan (formerly ACT-064992; ACT064992; ACT 064992; Opsumit) is an orally bioavailable and non-peptide, dual antagonist of ETA/ETB endothelin (ET) receptor. |
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V30150 | Macitentan n-butyl analogue | 556797-16-1 | Macitentan n-butyl analogue, an n-butyl derivative of Macitentan, is an ETA/ETB endothelin (ET) receptor dual antagonist that haspotential usefulness in the treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). |
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V75334 | Nebentan potassium (YM598) | 342005-82-7 | Nebentan potassium (YM598) is a potent, orally bioactive, non-peptide endothelin receptor (ETA receptor) antagonist modified by Bosentan. |
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V75340 | Patecibart | 2642374-04-5 | Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody (mAb). |
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V3337 | RO 46-8443 | 175556-12-4 | RO 46-8443 is a novel, potent, selective and non-peptidic antagonist of the endothelin ETB receptor. |
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V7251 | RO462005 | 150725-87-4 | Ro 46-2005 is a novel non-peptide endothelin antagonist that can inhibit human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM. |
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V81357 | Sarafotoxin S6a TFA | Sarafotoxin S6a TFA is a Sarafotoxin analogue and an endothelin receptor agonist/activator with similar ETA/ETB selectivity to Endothelin-3. | |
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V1511 | Sitaxentan sodium (Sitaxsentan; IPI 1040) | 210421-74-2 | Sitaxentan sodium (formerly IPI-1040; TBC-11251; IPI 1040; TBC11251; Thelin), the sodium salt ofSitaxentan, is a selective and orally bioavailable endothelin A receptor (ETA) antagonist with anti-hypertensive activity. |
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V1508 | Zibotentan (ZD4054) | 186497-07-4 | Zibotentan (formerly known as ZD-4054; ZD4054) is a specific and orally bioavailable Endothelin (ET)A antagonist with potential antitumor activity. |
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