Endothelin Receptor

Clazosentan (Ro 61-1790) is a selective antagonist of the endothelin A receptor (ETAreceptor) that inhibits ET-1-mediated vasoconstriction, preventing cerebral vasospasm and vasospasm-associated cerebral infarction.

Atrasentan (ABT-627) is an endothelin receptor antagonist that can inhibit the activity of ETA (IC50 value is 0.0551 nM).

Avosentan(Ro 67-0565; SPP-301) is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2]

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.

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.

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)

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.

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

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.

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

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.

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.

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

Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate is an atrial natriuretic peptide (ANP) hormone secreted by atrial myocytes that is capable of acting as an natriuretic peptide receptor-A(NPR-A) agonist, used in the treatment of acute decompensated heart failure (ADHF). By binding to specific receptors on the surface of the kidney, blood vessel, and heart cells, Carperitide causes an increase in cyclic guanosine monophosphate (cGMP) levels and induces vasodilatation, diuresis, and sodium excretion, which in turn reduces the heart's workload.

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.

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.

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).

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.

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

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

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.

Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).

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

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

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

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

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.

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

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.

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.

IRL-1038 TFA is a selective and potent endothelin B (ETB) receptor antagonist that inhibits endothelin-induced endothelium-dependent relaxation and can be used in the study of cardiovascular disease.

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

Macitentan-d4 (ACT-064992 D4) is a deuterated substitute for Macitentan and can be used as a dual antagonist of the non-peptides ETA and ETB (endothelin receptor).Macitentan-d4 is less toxic than Macitentan, has a longer half-life, and can be used to study endothelin receptor-mediated diseases.

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

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

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, critically regulates blood pressure, fluid balance, and electrolyte homeostasis [1] [2].

Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of the ETA receptor with an IC50 of 0.26 μM.