Endothelin Receptor

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

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.

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.

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)

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.

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.

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

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.

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

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.

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]

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.

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

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.

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.

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

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

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).

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).

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

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.

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 endothelin receptor antagonist with an IC50 of 55.1 μM for ETA.