eta and etb

Endothelin 1 (swine, human) is a potent endogenous vasoconstrictor peptide released primarily by endothelial cells and acting through ETA and ETB receptors. Endothelin 1 (swine, human) mediates vascular smooth-muscle contraction, promotes fibrosis, stimulates reactive oxygen species production, and induces pro-inflammatory signaling, making it central to studies of vascular dysfunction, hypertension, and oxidative stress–associated pathology.

N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met inhibits endothelin binding to membranes from CHO cells carrying human ETA receptor and human ETB receptor with IC50 of 268nM and 1810nM, respectively.

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.

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.

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA/ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

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.

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

PD-159020 is a non-selective antagonist of ETA/ETB (hETA and hETB) with IC50 values of 30 nM and 50 nM, respectively.

A-192621 is a potent, nonpeptide, orally active, and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and elevates both arterial blood pressure and plasma ET-1 levels[1][2][3]. Its selectivity is 636-fold higher for ETB than ETA (IC50 of 4280 nM and Ki of 5600 nM).

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.

Tezosentan is an antagonist of the endothelin receptor (pA2s: 9.5, 7.7 for ETA and ETB receptors, 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.

O-Deshydroxyethyl bosentan is a metabolite of bosentan, which is a competitive dual antagonist of endothelin-1 (ET) at both ETA and ETB receptors.

ENDOTHELIN-1 (ET-1), the principal peptide of the endothelin family, has been shown to have a variety of biological activities in both vascular and nonvascular tissues. The C-terminal fragment, which is a highly conserved sequence in the peptides of t

Ac-Endothelin-1 (16-21), human acetate, the principal peptide of the endothelin family, has been shown to have a variety of biological activities in both vascular and nonvascular tissues. The C-terminal fragment, which is a highly conserved sequence in th

J-104132 is a potetn and selective endothelin A/B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova

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.

Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner,Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].In measurement of intracellular Ca2+ concentration, Nebentan concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1]. Nebentan (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan (oral administration; 1 mg/kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. [1]. Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71. [2]. Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S354-7.

Sclerotiorin is a natural product isolated primarily from Penicillium species. It inhibits soybean lipoxygenase-1 with an IC50 value of 4.2 μM. Sclerotiorin also exhibits a number of other activities including inhibition of cholesterol ester transfer protein (IC50 = 19.4 μM),, inhibition of Grb2-Shc interaction (IC50 = 22 μM),, and antagonism of endothelin receptors (IC50 = 114 and 152 μM for human ETA and ETB, respectively).

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

Bosentan-d4, the deuterium-labeled variant of Bosentan, serves as a competitive dual antagonist against endothelin-1 (ET) by targeting both ET A and ET B receptors. It exhibits binding affinities with K i values of 4.7 nM for ET A and 95 nM for ET B in human SMC.

Endothelin 1 (swine, human) (TFA) is a synthetic peptide mirroring the sequence of the potent endogenous vasoconstrictor found in both human and swine Endothelin 1, operating via two receptor types, ET A and ET B [1].

Endothelin 1 (swine, human), Alexa Fluor 488-labeled, is a synthetic peptide mirroring human and swine Endothelin 1, an endogenous vasoconstrictor, and is tagged with Alexa Fluor 488 for fluorescence, operating via two receptor types, ET A and ET B [1].

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