endothelin b receptor

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.

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.

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.

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

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.

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.

DEDN6526A (RG-7636) is a humanized ADC compound targeting endothelin B receptor (ETBR), which can be used to study melanoma.

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

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

Vodudeutentan is an antagonist of the immune checkpoint endothelin B receptor (ETBR; EDNRB) and possesses potential immunoregulatory and antitumor properties.

Vodudeutentan acts as an antagonist of the endothelin B receptor (ETBR; EDNRB), and has potential immunomodulatory and antitumor activities.

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

L-749329 is a ligand of ET(A) and ET(B) endothelin receptor.

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).

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.

BE-24566B is a polyketide fungal metabolite originally isolated fromS. violaceusniger.1It is active againstB. subtilis,B. cereus,S. aureus,M. luteus,E. faecalis, andS. thermophilus(MICs = 1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/ml, respectively). BE-24566B is an endothelin (ET) receptor antagonist (IC50s = 11 and 3.9 μM for ETAand ETBreceptors, respectively).2 1.Kojiri, K., Nakajima, S., Fuse, A., et al.BE-24566B, a new antibiotic produced by Streptomyces violaceusnigerJ. Antibiot. (Tokyo)48(12)1506-1508(1995) 2.Lam, Y.K.T., Hensens, O., Helms, G., et al.L-755,805, a new polyketide endothelin binding inhibitor from an actinomyceteTetrahedron Lett.36(12)2013-2016(1995)

Sulfisoxazole diethanolamine, also known as Sulfafurazole diethanolamine, is a sulfonamide antibacterial compound with an oxazole substituent. It acts as an endothelin receptor antagonist, specifically targeting endothelin receptor A with an IC50 value of 0.60 μM and endothelin receptor B with an IC50 value of 22 μM. Additionally, Sulfisoxazole diethanolamine has been found to inhibit the release of breast cancer exosomes by specifically targeting endothelin receptor A [1] [2].

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].

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].

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