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Endothelin Receptor

Endothelin Receptor

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.

Endothelin Receptor related products

Structure Cat No. Product Name CAS No. Product Description
[Ala1,3,11,15]-Endothelin (53-63) (TFA) 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 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 (swine, human) V122410 [Asn18] Endothelin-1 (swine, human) 138716-98-0 [Asn18] Endothelin-1 (swine, human) is a structural analog of porcine endothelin-1 and human endothelin-1, in which the Asp amino acid at position 18 is mutated to Asn.
[Asn18] Endothelin-1, human V75341 [Asn18] Endothelin-1, human 309245-97-4 [Asn18] Endothelin-1, human is a polypeptide.
[Lys4] Sarafotoxin S6c V75338 [Lys4] Sarafotoxin S6c 1219444-22-0 [Lys4] Sarafotoxin S6c is a sarafotoxin analogue and a potent partial agonist of the endothelin receptor.
ACT-373898 V75337 ACT-373898 1433875-14-9 ACT-373898 is an inactive carboxylic acid metabolite of Macitentan.
ANP (1-30), frog V75335 ANP (1-30), frog 309245-16-7 ANP (1-30), frog is a polypeptide fragment of frog-derived atrial peptide.
Aselacin A V129492 Aselacin A 156223-06-2 Aseracin A targets the endothelin-1 receptor (ET-1 receptor) and inhibits the binding of ET-1 to the ETA and ETB receptors.
Aselacin B V129493 Aselacin B 156223-07-3 Aseracin B targets the endothelin-1 receptor (ET-1 receptor) and inhibits the binding of ET-1 to the ETA and ETB receptors.
Atrasentan sodium V93978 Atrasentan sodium 178738-96-0 Atrasentan sodium is a potent endothelin receptor antagonist that inhibits the activity of ETA with an IC50 value of 0.0551 nM.
Atrial natriuretic peptide (3-28) (human) (ANP (3-28) (human)) 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.
Atrial natriuretic Peptide (ANP) (1-28), rat TFA (Atrial natriuretic factor (1-28) (rat) TFA) 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.
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA V129629 Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA is the main circulating form of ANP in rats, which can effectively inhibit the secretion of angiotensin II (Ang II)-stimulated endothelin-1 in a concentration-dependent manner.
Big endothelin-3 (Human, 1-41 amide) V110580 Big endothelin-3 (Human, 1-41 amide) 133551-97-0 Large endothelin-3 (human, 1-41 amide) is a precursor molecule of the endothelin-3 (ET-3) peptide, consisting of 41 amino acids.
Bosentan-d4 V75336 Bosentan-d4 1065472-77-6 Bosentan-d4 is the deuterium labelled form of Bosentan.
BQ-123 TFA 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.
BQ-3020 ammonium V77187 BQ-3020 ammonium BQ-3020 ammonium is an endothelin receptor (ETBreceptor) agonist.
BQ-610 V115628 BQ-610 141595-53-1 BQ-610 is a selective endothelin A receptor (ETA receptor) antagonist.
Cgs 27830 V131454 Cgs 27830 155485-56-6 Cgs 27830 is an endothelin receptor antagonist with 20 times higher selectivity for ET-A receptors than for ET-B receptors.
CI-1020 (PD156707) 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.
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