Date published: 2026-2-22

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NPY4-R Activators

Chemical activators of NPY4-R include a variety of compounds that engage with this receptor to initiate a cascade of biological responses. Pancreatic Polypeptide, a natural agonist of NPY4-R, binds directly to the receptor, enabling its role in controlling gut motility and the secretion of pancreatic enzymes. Similarly, the synthetic peptide BVD-10 acts as a small-molecule agonist, directly interacting with NPY4-R to exert influence on physiological functions such as the regulation of food intake. Analog peptides like [Leu31, Pro34]NPY also target NPY4-R and are known to activate it, subsequently affecting energy homeostasis. Continuing with the chemical activators, Ac-RYYRWK-NH2, a hexapeptide analog of neuropeptide FF, activates NPY4-R, triggering signal transduction pathways that are associated with appetite control and energy balance. BIBO3304 and GR231118, while functioning as antagonists at other neuropeptide receptors, have been reported to activate NPY4-R, suggesting a unique and selective activation pattern that targets this receptor. Additionally, JNJ-31020028, primarily an antagonist at NPY2-R, may evoke an agonistic effect on NPY4-R, leading to receptor activation. Lastly, LY-255582, which is an antagonist at NPY1-R, has been reported to functionally activate NPY4-R, highlighting the complex interaction dynamics that can occur between different ligands and the receptor, leading to its activation and subsequent biological responses.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

GR 231118

158859-98-4sc-361194
500 µg
$345.00
1
(0)

GR 231118 functions as a selective antagonist for the NPY4 receptor, distinguished by its ability to engage in specific electrostatic interactions with key amino acid residues within the receptor's binding pocket. Its unique structural features promote a conformational shift in the receptor, effectively disrupting typical signaling pathways. This compound's kinetic profile reveals a rapid association and slower dissociation, underscoring its potential for prolonged receptor modulation.