Date published: 2025-12-24

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urocortin (UCN) Inhibitors

Urocortin (UCN) inhibitors represent a class of chemical compounds designed to modulate the activity of urocortin peptides. Urocortins are a group of neuropeptides that belong to the corticotropin-releasing factor (CRF) family and are involved in a wide array of physiological processes, including stress response, metabolic regulation, and cardiovascular function. These peptides, including UCN1, UCN2, and UCN3, bind to specific receptors known as CRF receptors (CRFR1 and CRFR2), triggering various downstream signaling pathways. Urocortin inhibitors act by blocking or reducing the interaction between urocortins and these receptors, thereby modulating the biological effects induced by urocortin signaling. Such inhibitors are typically small molecules, peptides, or antibodies that target specific binding sites on urocortin peptides or their receptors, preventing conformational changes or binding necessary for receptor activation.

The design and development of urocortin inhibitors require a deep understanding of the structural biology of the CRF family peptides and their receptors. This involves extensive research on the binding kinetics and affinities of urocortins to their receptors, as well as the identification of key amino acid residues critical for receptor-ligand interaction. By studying the molecular interactions between urocortins and CRF receptors, researchers can identify potential points of intervention, leading to the development of more specific and selective inhibitors. Moreover, the role of these inhibitors in altering intracellular signaling pathways, such as cyclic adenosine monophosphate (cAMP) production or calcium ion mobilization, is crucial in understanding the broader physiological effects of blocking urocortin activity. Through this approach, urocortin inhibitors contribute to expanding the knowledge of the underlying biochemical mechanisms involved in various physiological functions controlled by the CRF family peptides.

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A non-peptide CRF receptor antagonist, particularly targeting CRF1 receptor, used in research to study stress-related responses.