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, 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.
Ambrisentan (BSF 208075; LU 208075) 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).
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.
Atrasentan 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.
Atrasentan HCl 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.
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.
Bosentan 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.
Bosentan Hydrate (Ro 47-0203) 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.
Bosentan-d4 V75336 Bosentan-d4 1065472-77-6 Bosentan-d4 is the deuterium labelled form of Bosentan.
BQ-123 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.
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.
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.
Edonentan hydrate (BMS 207940 hydrate) V85769 Edonentan hydrate (BMS 207940 hydrate) 264609-13-4
Endothelin 1 (swine, human) (TFA) 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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