Date published: 2026-4-29

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ETAR Inhibitors

ETAR inhibitors belong to a chemical class of compounds or substances that are designed to modulate the activity of the Endothelin A receptor (ETAR). ETAR is a G protein-coupled receptor that is part of the endothelin receptor family. Activation of ETAR by its ligand, endothelin-1, triggers a cascade of cellular responses involved in various physiological processes. ETAR inhibitors are specifically designed to interact with ETAR and interfere with its function. By binding to ETAR, these inhibitors can block the binding of endothelin-1 and subsequent activation of the receptor. This inhibition of ETAR can affect downstream signaling pathways and attenuate the effects of endothelin-1 on cellular processes. Some examples of ETAR inhibitors include bosentan, ambrisentan, macitentan, zibotentan, and atrasentan. The development and study of ETAR inhibitors contribute to a deeper understanding of the role of ETAR in various physiological and pathological processes. Further research is required to fully characterize the properties, mechanisms of action, and potential applications of ETAR inhibitors.

Items 11 to 14 of 14 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Sitaxsentan Sodium

210421-74-2sc-215857
10 mg
$640.00
(0)

Sitaxsentan Sodium, as an ETAR, exhibits a unique mechanism of action through its selective antagonism of endothelin-1, leading to altered receptor dynamics. Its molecular structure allows for specific hydrogen bonding and hydrophobic interactions, enhancing its affinity for the receptor. The compound's kinetic properties facilitate rapid receptor occupancy, influencing the downstream signaling cascade. Additionally, its solubility profile supports effective membrane permeability, optimizing its interaction with target sites.

PD 151,242

155561-67-4sc-215681
200 µg
$52.00
(0)

PD 151,242 functions as an ETAR by selectively modulating receptor activity through its unique structural conformation, which promotes specific electrostatic interactions. This compound demonstrates distinct reaction kinetics, allowing for a rapid onset of action and prolonged receptor engagement. Its ability to form stable complexes with the receptor enhances signal transduction efficiency. Furthermore, PD 151,242's lipophilic characteristics contribute to its effective membrane integration, facilitating targeted interactions within cellular environments.

Bosentan-d4

sc-217787
1 mg
$320.00
(1)

Bosentan-d4 acts as an ETAR by engaging in selective binding that alters receptor conformation, leading to unique allosteric modulation. Its isotopic labeling enhances tracking in metabolic studies, providing insights into receptor dynamics. The compound exhibits distinctive solubility properties, promoting effective diffusion across lipid membranes. Additionally, Bosentan-d4's kinetic profile reveals a nuanced interaction with downstream signaling pathways, influencing cellular responses in a targeted manner.

Macitentan

441798-33-0sc-489332
sc-489332A
5 mg
25 mg
$320.00
$440.00
(0)

Macitentan functions as an ETAR through its ability to selectively inhibit receptor activity, resulting in a shift in signaling cascades. Its unique structural features facilitate strong interactions with the receptor's binding site, promoting a stable complex formation. The compound's lipophilic nature enhances its permeability through biological membranes, while its kinetic behavior indicates a prolonged duration of action, allowing for sustained modulation of receptor-mediated pathways.