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 |
---|---|---|---|---|
V77466 | [Ala1,3,11,15]-Endothelin (53-63) (TFA) | [Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. | ||
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. | |
V75341 | [Asn18] Endothelin-1, human | 309245-97-4 | [Asn18] Endothelin-1, human is a polypeptide. | |
V75338 | [Lys4] Sarafotoxin S6c | 1219444-22-0 | [Lys4] Sarafotoxin S6c is a sarafotoxin analogue and a potent partial agonist of the endothelin receptor. | |
V75337 | ACT-373898 | 1433875-14-9 | ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. | |
V75335 | ANP (1-30), frog | 309245-16-7 | ANP (1-30), frog is a polypeptide fragment of frog-derived atrial peptide. | |
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. | |
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. | ||
V75336 | Bosentan-d4 | 1065472-77-6 | Bosentan-d4 is the deuterium labelled form of Bosentan. | |
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. | ||
V77187 | BQ-3020 ammonium | BQ-3020 ammonium is an endothelin receptor (ETBreceptor) agonist. | ||
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. | |
V86600 | Clazosentan disodium | 503271-02-1 | Clazosentan disodium (Ro 61-1790) is a selective endothelin A receptor (ETA receptor) antagonist. | |
V85769 | Edonentan hydrate (BMS 207940 hydrate) | 264609-13-4 | ||
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. | |
V79302 | Endothelin 1 (swine, human), Alexa Fluor 488-labeled | Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic peptide of Endothelin 1 labeled with 488 fluorescence. | ||
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. | ||
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. | ||
V86599 | Methylsolfonyl 25(S)-Δ7-dafachronic acid | Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with IC50 of 0.41 μM. | ||
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. |