Endothelin Receptor

Avosentan (Ro 67-0565) is an effective and selective antagonist of the endothelin receptor (ETA receptor).

Enrasentan (sb-217242) is a mixed antagonist of ET(A) and ET(B) receptors that reduces blood pressure, prevents cardiac hypertrophy, and protects myocardial function.

Sitaxsentan (TBC-11251) is A selective endothelin A (ETA) receptor antagonist. Endothelin is an effective vasoconstrictor. Sitaxsentan blocks the binding of endothelin to its receptors, thereby eliminating the harmful effects of endothelin.

SB-209670 is a selective endothelin receptor antagonist that inhibits the activity of ET(B) receptors in rat vascular endothelium and vascular smooth muscle.

Endothelin 1 (swine, human) acetate is a synthetic peptide with the sequence of human and swine Endothelin 1. Endothelin 1 is a potent endogenous vasoconstrictor and acts through two types of receptors ETA and ETB.

Edonentan is A potent endothelin A (ETA) receptor antagonist that can be used to study heart failure.

Aminaftone, a derivative of 4-aminobenzoic acid, inhibits endothelin-1 (ET-1) production and can be used to study hypertension and systemic sclerosis.

IRL-1038 acetate is a potent ETB endothelin receptor antagonist.

IRL-1620 acetate is an effective and selective agonist of Endothelin B receptor (ETB) with a Ki of 16 pM which is more selective than ETA with a Ki of 19 μM.

BMS 182874 hydrochloride is a nonpeptide endothelin (El) receptor antagonist.

Nebentan potassium (YM598) is an orally active and selective nonpeptide endothelin receptor (ETA receptor) antagonist.Nebentan potassium inhibits pulmonary arterial hypertension and may be useful in the study of neurologic and cardiovascular diseases.

Clazosentan (Ro 61-1790) is a specific endothelin A (ETA) receptor antagonist that inhibits ET-1-mediated vasospasm.Clazosentan is used in the study of neurological and cardiovascular diseases.

BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.

Atrasentan (ABT-627) (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).

Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension.

Ro 46-2005 is a synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor, IC50: 220 nM).

Patecibart is a humanized immunoglobulin G4-kappa monoclonal antibody that functions as an antagonist to the endothelin receptor A (EDNRA).

Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.

Myriceric acid C has cytotoxic activity against human lung carcinoma and breast carcinoma.

Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

Sparsentan (DARA-a) is a first-in-class orally active and highly potent dual endothelin A and angiotensin II receptor antagonist(Ki of 9.3 and 0.8 nM, respectively)

Aprocitentan (ACT-132577) is ETA and ETB antagonist .

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition.

Bosentan hydrate (Ro 47-0203) is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.

Darusentan (Lu-135252) is a potent inhibitor of endothelin signaling and function in both large and small arteries

BQ-3020 ammonium, a selective endothelin receptor (ET B receptor) agonist, demonstrates inhibition of [125 I] ET-1 binding to ET B receptors with an IC50 of 0.2 nM and induces vasoconstriction in rabbit pulmonary arteries. Additionally, it promotes relaxation of the pig urinary bladder neck, rendering it useful for research into cardiovascular diseases [1] [2].

Atrial natriuretic peptide (3-28) (human) (ANP (3-28) (human)), a peptide hormone produced by the atrial myocardium, plays a critical role in the regulation of blood pressure, fluid balance, and electrolyte homeostasis [1] [2].

IRL 2500 is an antagonist of Endothelin receptor with IC50s of 1.3 and 94 nM for Endothelin A receptor and Endothelin B receptor.

Atrasentan hydrochloride (ABT-627 hydrochloride) is an antagonist of the endothelin receptor(IC50 = 55.1 μM for ETA).

Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate), a 28-amino acid hormone, is naturally produced and released by the human heart upon cardiac injury or mechanical stretch. This compound effectively inhibits the secretion of endothelin-1 in a dose-dependent manner.

Sulfisoxazole (Sulfafurazole) is a short-acting sulfonamide antibacterial with activity against a wide range of gram-negative and gram-positive organisms.Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.

Sitaxsentan sodium (TBC11251 sodium salt) is a highly selective antagonist of endothelin A receptors.

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

BMS 182874 is an orally effective and highly selective endothelin receptor ETA antagonist with an IC50 value of 0.150 μM for ETA and a Ki value of 0.055 μM for ETA.BMS 182874 is able to reduce arterial pressure in a rat hypertension model induced by Deoxycorticosterone acetate. BMS 182874 was able to reduce Deoxycorticosterone-induced arterial pressure in a rat model of hypertension and can be used to study cardiovascular disease.

Macitentan (ACT-064992) is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension (PAH).