endothelin receptor

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.

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

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

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.

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

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

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.

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].

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].

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

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

Aselacin A targets the endothelin-1 receptor (ET-1 Receptor) and inhibits the binding of ET-1 to both ETA and ETB receptors. It effectively impedes the binding of ET-1 to bovine atrial membranes and porcine brain membranes, with IC50 values of 22 μg mL and 20 μg mL, respectively. Aselacin A is applicable for cardiovascular disease research.

Aselacin B targets the endothelin-1 receptor (ET-1 Receptor) and inhibits the binding of ET-1 to both ETA and ETB receptors. It is used in cardiovascular disease research.

K-8794 is an orally active and selective endothelin receptor ETB antagonist that can be utilized in cardiovascular disease research.

RES-701-1 is a cyclic peptide consisting of 16 common L-amino acids. It acts as a specific antagonist of the ETB receptor. RES-701-1 inhibits the binding of 125I-ET-1 (125I-labeled endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM.

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

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

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

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.

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.

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).