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 |
|---|---|---|---|---|
![[Ala1,3,11,15]-Endothelin (53-63) (TFA)](http://www.invivochem.com/upload/1124/V77466.png)
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V77466 | [Ala1,3,11,15]-Endothelin (53-63) (TFA) | [Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. | |
![[Ala2] Endothelin-3, human](http://www.invivochem.com/upload/1124/V75339.png)
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V75339 | [Ala2] Endothelin-3, human | 2243207-08-9 | [Ala2] Endothelin-3, human is a linear analog of endothelin ET-3 in which Ala replaces the Cys residue. |
![[Asn18] Endothelin-1, human](http://www.invivochem.com/upload/1124/V75341.png)
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V75341 | [Asn18] Endothelin-1, human | 309245-97-4 | [Asn18] Endothelin-1, human is a polypeptide. |
![[Lys4] Sarafotoxin S6c](http://www.invivochem.com/upload/1124/V75338.png)
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V75338 | [Lys4] Sarafotoxin S6c | 1219444-22-0 | [Lys4] Sarafotoxin S6c is a sarafotoxin analogue and a potent partial agonist of the endothelin receptor. |
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V75337 | ACT-373898 | 1433875-14-9 | ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. |
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V1512 | Ambrisentan (BSF 208075; LU 208075) | 177036-94-1 | Ambrisentan (formerly BSF-208075; LU-208075; BSF208075; LU208075; Letairis; Volibris; pulmonext) is a selective antagonist of the endothelin-1 type A receptor (ETA). |
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V75335 | ANP (1-30), frog | 309245-16-7 | ANP (1-30), frog is a polypeptide fragment of frog-derived atrial peptide. |
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V4421 | Atrasentan | 173937-91-2 | Atrasentan (ABT-627; NSC720763; A-147627; trade name: Xinlay) is a novel, selective and potent endothelin receptor/ET antagonist with anticancer activity. |
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V4422 | Atrasentan HCl | 195733-43-8 | Atrasentan HCl, the hydrochloride salt of Atrasentan (NSC-720763; ABT-627; A-147627; trade name: Xinlay), is a novel and selective endothelin receptor antagonist (IC50 = 0.0551 nM for ETA) with anticancer activity. |
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V75342 | Atrial natriuretic peptide (3-28) (human) (ANP (3-28) (human)) | 102686-43-1 | Atrial natriuretic peptide (3-28) (human) (ANP (3-28) (human)) is a bioactive peptide hormone synthesized and secreted by the atrial myocardium. |
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V77230 | Atrial natriuretic Peptide (ANP) (1-28), rat TFA (Atrial natriuretic factor (1-28) (rat) TFA) | Atrial Natriuretic Peptide (ANP) (1-28), rat (TFA) is the major circulating form of atrial natriuretic peptide (ANP) in rats and potently inhibits angiotensin II (Ang II)-stimulated endothelin- 1 (endothelin-1) secretion. | |
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V1513 | Bosentan | 147536-97-8 | Bosentan (formerly Ro 47-0203; brand name Tracleer) is a potent, competitive and dual antagonist of endothelin (ET) receptor with anti-hypertensive activity. |
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V1509 | Bosentan Hydrate (Ro 47-0203) | 157212-55-0 | Bosentan Hydrate (also known as Ro 47-0203; Ro47-0203; Ro-47-0203; Tracleer) is a potent, competitive and dual endothelin (ET) A/B receptor antagonist for ET-A and ET-B with anti-hypertensive activity. |
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V75336 | Bosentan-d4 | 1065472-77-6 | Bosentan-d4 is the deuterium labelled form of Bosentan. |
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V1514 | BQ-123 | 136553-81-6 | BQ-123 (Cyclo(D-trp-D-asp-pro-D-val-leu); BQ123; BQ 123) is a potent andselective antagonist of endothelin A receptor (ETAR) with an IC50 of 7.3 nM. |
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V78540 | BQ-123 TFA | BQ-123 TFA is a potent and specific endothelin A (ETA) receptor antagonist (inhibitor) with IC50 of 7.3 nM and a Ki of 25 nM. | |
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V77187 | BQ-3020 ammonium | BQ-3020 ammonium is an endothelin receptor (ETBreceptor) agonist. | |
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V75333 | CI-1020 (PD156707) | 162256-50-0 | CI-1020 (PD156707) is an orally bioactive selective antagonist targeting endothelin (ETA) with IC50 of 0.3 nM. |
|
V85769 | Edonentan hydrate (BMS 207940 hydrate) | 264609-13-4 | |
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V75332 | Endothelin 1 (swine, human) (TFA) | 394693-38-0 | Endothelin 1 (swine, human) (TFA) is a synthetic peptide with the sequence of human and porcine endothelin 1 and is a potent endogenous vasoconstrictor. |
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