Urantide acts as selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3), which blocks hU-II induced contractions in thoracic aorta ex vivo, and has no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. It behaves as a partial agonist in a calcium mobilization assay (in CHO cells expressing hUT receptors).
CAT No: R1053
CAS No:669089-53-6
Synonyms/Alias:URANTIDE;669089-53-6;(2S)-2-[[(4R,7S,10S,13R,16S,19S)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-10-(3-aminopropyl)-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid;(Pen5,DTrp7,Orn8)U-II (4-11) (human);[Pen5,DTrp7,Orn8]U-II (4-11) (human);CHEMBL223905;BDBM50411333;AKOS025147344;(Pen(5),DTrp(7),Orn(8))hU-II(4-11);
Urantide is a synthetic peptide and selective antagonist of the urotensin II receptor (UT receptor), recognized for its pivotal role in modulating the urotensinergic signaling pathway. As a cyclic peptide analog of urotensin II, urantide has garnered significant attention in biochemical and pharmacological research due to its high affinity for the UT receptor and its ability to inhibit downstream signaling events. Its precise mechanism of action and receptor specificity make it a valuable molecular tool for dissecting the physiological and pathophysiological roles of urotensin II, a peptide implicated in diverse cellular processes such as vasoregulation, cell proliferation, and neuroendocrine modulation. The availability of urantide as a research-grade compound enables in-depth investigation into the urotensin II system, supporting a broad spectrum of experimental applications in molecular biology, pharmacology, and peptide science.
Receptor antagonist studies: As a potent UT receptor antagonist, urantide is extensively utilized in receptor binding and signal transduction assays to elucidate the functional consequences of urotensin II receptor blockade. By competing with endogenous urotensin II for receptor occupancy, it enables researchers to delineate the specific contributions of UT receptor signaling to cellular responses in cardiovascular, renal, and central nervous system models. This application is critical for mapping downstream pathways activated by urotensin II and for validating the receptor as a target in basic and translational research.
Vasoregulatory research: The compound's ability to inhibit urotensin II-induced vasoconstriction underpins its frequent use in studies of vascular tone regulation. In isolated tissue preparations and ex vivo vascular models, urantide provides a means to assess the role of the urotensinergic system in modulating arterial contractility, endothelial function, and smooth muscle cell behavior. These investigations contribute to a deeper understanding of the mechanisms governing blood pressure control and vascular homeostasis at the molecular level.
Cell signaling pathway analysis: Urantide serves as a critical tool for probing intracellular signaling cascades triggered by UT receptor activation. By selectively blocking urotensin II-mediated effects, it facilitates the dissection of G protein-coupled receptor (GPCR) pathways, including those involving calcium mobilization, MAPK activation, and gene transcription. Its use in cellular assays enables precise attribution of observed signaling events to UT receptor engagement, thereby supporting the characterization of pathway specificity and cross-talk with other receptor systems.
Peptide structure-activity relationship (SAR) studies: The unique cyclic structure and receptor affinity profile of urantide make it an informative reference compound for SAR investigations within the urotensin II peptide family. Researchers employ it as a benchmark to compare the binding kinetics, conformational features, and functional activities of novel peptide analogs or modified sequences. Such studies advance the rational design of next-generation UT receptor modulators and contribute to the broader field of peptide-based drug discovery.
In vivo functional assays: In preclinical research settings, urantide is applied in animal models to assess the physiological impact of UT receptor antagonism on systemic and organ-specific functions. Its use enables the evaluation of urotensinergic involvement in processes such as hemodynamic regulation, stress responses, and neuroendocrine signaling. These studies provide foundational insights that inform future investigations into the biological significance of the urotensin II system, supporting the ongoing development of selective receptor modulators for research purposes.
In vivo daily administration of urantide for three days resulted in reduced blood TG, TC, HDL and LDL levels in rat aortic tissue, in addition to the downregulation of the expression of the inflammatory mediators CRP and MCP-1, thus improving the symptoms of AS. These effects were identified to be time-dependent.
Urantide improves atherosclerosis by controlling C reactive protein, monocyte chemotactic protein 1 and transforming growth factor-β expression in rats
Urantide, a hU-II analogue, is a potent UT receptor antagonist that could block hU-II-induced contractions in the rat isolated thoracic aorta and displaces 125I-hU-II binding on UT receptor transfected CHO/K1 cells. Though our preliminary studies have shown that urantide had a protective effect against myocardial IR injury in rats and mice, the cardioprotection property needed to be confirmed by further study. The post-receptorial mechanism of urantide on myocardial IR injury is still not clear. It is currently known that protein kinase C (PKC) and phosphtidylinositol 3′-kinase – Akt (PI3K–Akt) signaling pathways are involved in protection against myocardial IR injury. The present study was therefore designed to confirm the protective effect of urantide against myocardial IR injury in rats and to investigate whether PKC and PI3K–Akt signaling pathways are involved in the protective effects of urantide.
Protective effect of urantide against ischemia–reperfusion injury via protein kinase C and phosphtidylinositol 3′-kinase – Akt pathway
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