Aminaftone, a derivative of 4-aminobenzoic acid, downregulatesendothelin-1(ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
Atrial Natriuretic Peptide ...
Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulatedendothelin-1secretion in a concentration-dependent manner.
Endothelin 1 (swine, human)
Endothelin 1 (swine, human) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB.
Sarafotoxin S6a, a sarafotoxin analogue, is aendothelin receptoragonist and has anETA/ETBselectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC50 value o...
Bosentan is a competitive and dual antagonist ofendothelin-1 (ET)for the ETA and ETBreceptors with Kiof 4.7nM and 95nM in human SMC, respectively.
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220nM.
BQ-788 sodium salt
BQ-788 sodium salt is a potent and selectiveETB receptorantagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2nM in human Girrardi heart cells.
IRL 2500 is a potentEndothelin receptorantagonist. IRL 2500 showsIC50 values of 1.3 and 94nM for ETB and ETAreceptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascu...
Darusentan (Lu-135252) is a selectiveendothelin receptor A(ET-A)receptorantagonist, which binds with a Ki of 1.4nM to the ET-A receptor and a Kiof 184nM to ET-B receptor, respectively with a 100-fold selectivity for ETA...
BQ-788 is a potent, selectiveETB receptorantagonist with IC50 of 1.2nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC c...
Ambrisentan is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).
Tezosentan (RO 610612) is anendothelin (ET)receptor antagonist, withpA2sof 9.5, 7.7 for ETA and ETBreceptors, respectively.
Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.
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