Macitentan is an orally active, non-peptide endothelin receptor antagonist for the treatment of idiopathic pulmonary fibrosis and pulmonary arterial hypertension.
Macitentan D4 (ACT-064992 D4) is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan is used for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). IC50 value: 21 nM Target: ETA receptorZibotentan is capable of inhibiting or reducing the multitude of effects that are evoked by ET-1 activation of the ETA receptor and which promote tumor survival, growth and progression. Zibotentan (ZD4054) treatment produced significant inhibition of tumor growth in ovarian and breast xenografts.
ANP (1-30), frog is a peptide fragment of atrial natriuretic peptide derived from frog. ANP (1-30), frog has natriuretic, diuretic, and vasorelaxant effects.
Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is ＞25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively[1].
ACT-132577 is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.
Tezosentan-d4 (RO 610612-d4) is the deuterium labeled Tezosentan. Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively[1][2].
Sulfisoxazole, an endothelin receptor antagonist, is a sulfonamide antibacterial with an oxazole substituent.Target: Antibacterial; Endothelin ReceptorThe sulfanilamide antibacterial agent sulfisoxazole was found to be a good endothelin receptor antagonist (IC50's of 0.60 microM and 22 microM for the ETA and ETB receptors, respectively) [1]. Sulfisoxazole is used to treat or prevent infections in many different parts of the body. It belongs to the group of medicines known as sulfonamide antibiotics. It works by preventing the growth of bacteria [2].
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].
BQ-788 (sodium salt) is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
[Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) where substitution of Ala for Cys residues. TE-3 is a vasoactive peptide, produced by human rhabdomyosarcoma cell lines, whereas it is not expressed by human sarcoma cell lines of non-muscle origin. ET-3 acts as a paracrine factor, since it promotes migration of endothelial cells[1][2].
Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
Atrial natriuretic peptide (3-28) (human) (ANP (3-28) (human)) is a peptide hormone that is synthesized and secreted by the atrial myocardium. Atrial natriuretic peptide (3-28) (human) is involved in the regulation of blood pressure, fluid balance, and electrolyte homeostasis[1][2].
Sarafotoxin S6c (SRTX-c) is a potent endothelin-B receptor agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels[1].
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction[1][5].
Avosentan(Ro 67-0565; SPP-301) is a potent, selective endothelin receptor(ETA receptor) antagonist.IC50 value:Target: ETA receptor
[Asn18] Endothelin-1, human is a peptide. Endothelin-1 is a major isoform of Endothelin and plays an important role for regulation of vascular function[1].
Vodudeutentan is an endothelin receptor antagonist[1].
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.
Sitaxsentan (IPI 1040; TBC 11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.IC50 value:Target: ETA receptor
Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an endothelin receptor antagonist[1].
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration[1][2][3].
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2].
Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively[1].