etb

ETB067, an H-89 analog, acts as a PKA and AKT1 inhibitor with specificity on no longer inhibiting CAMK2B and neither affecting viability of mice nor causing any detectable tissue damage at the dose given.

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).

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.

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

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.

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.

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

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.

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.

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.

Etbicyphat (Trimethylopropane phosphate), a potent competitive antagonist of GABA(A) receptors, binds to GABA(A)-benzodiazepine receptors and induces epileptiform activities in hippocampal CA1 neurons.

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.

[Ala1,3,11,15]-Endothelin (TFA) is a highly selective for endothelin A (ETA) and endothelin B (ETB) receptor.[Ala1,3,11,15]-Endothelin is a selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ET

ETB endothelin receptor antagonist

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

IRL-1620 (TFA) is a potent selective endothelin receptor B (ETB) agonist with a Ki value of 16pm.

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].

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.

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

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).

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.

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.

IRL-1620 (TFA) is a potent and selective agonist for the endothelin receptor type B (ETB) with an affinity (Ki) of 16 pM.

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].

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

Endothelin 1 (swine, human), a synthetic peptide mirroring the sequence of both human and swine Endothelin 1, functions as a robust endogenous vasoconstrictor by interacting with two receptor types, ETA and ETB.

BMS-193884 is an oral endothelin antagonist for the treatment of congestive heart failure (CHF) and pulmonary arterial hypertension.

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

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

BQ-788 sodium salt is a potent and selective antagonist of ETB receptor [ETB receptors] with an IC50 of 1.2 nM in human Girrardi heart cells.

BQ-3020 (TFA) is a selective ETB receptor agonist that inhibits [125I] et-1 binding to the ETB receptor in the cerebellum with a 0.2nm IC50, causing vasoconstriction.

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.

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

[Ala1,3,11,15]-Endothelin (53-63) (TFA) is a selective ET B agonist with IC50 values from 0.33 nM to 0.61 nM, indicating a high affinity for ET B receptors, and is used in vasoconstriction research.

Sarafotoxin S6a TFA, an analogue of sarafotoxin, functions as an endothelin receptor agonist with an ET_A/ET_B selectivity profile akin to Endothelin-3. It demonstrates an EC_50 of 7.5 nM in stimulating the pig coronary artery [1].

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.

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

BQ-3020 (TFA) is a selective ETB receptor agonist that inhibits [125I]ET-1 binding to the ETB receptor in the cerebellum with an IC50 of 0.2 nM and induces vasoconstriction [1].

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.

Selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ETB and ETA receptors respectively).

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).

IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM).

N-Despropyl Macitentan-d4 is a deuterated compound of N-Despropyl Macitentan. N-Despropyl Macitentan has a CAS number of 1103522-45-7. Aprocitentan is ETA and ETB antagonist .

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].

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).

Highly selective ETB endothelin receptor agonist (Ki values are 0.29 and 28000 nM at ETB and ETA receptors respectively).

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