Urotensin-II (UT) receptor antagonist. Unlike other U-II/URP analogs, it has no agonist activity.
[Orn5]-URP is a synthetic peptide analog of Urotensin II-related peptide (URP) in which the fifth amino acid position is substituted with ornithine. As a member of the urotensin peptide family, it is structurally engineered to probe the structure-activity relationships and functional properties of URP and its receptor interactions. The incorporation of ornithine at a key residue offers researchers a powerful tool for dissecting the molecular determinants of ligand binding, receptor activation, and downstream signaling of the urotensinergic system. Its defined sequence and modifiable nature make it highly relevant for studies in peptide pharmacology, receptor biology, and peptide engineering.
Receptor binding studies: [Orn5]-URP is widely utilized in receptor binding assays to investigate the affinity and selectivity of urotensinergic ligands for their cognate receptors, particularly the UT receptor (GPR14). The ornithine substitution allows researchers to evaluate the contribution of the fifth residue to receptor recognition and ligand-receptor interaction dynamics. By comparing the binding profiles of native URP and its analogs, such as [Orn5]-URP, scientists can map critical contact points within the peptide-receptor interface, thereby guiding the rational design of novel agonists or antagonists.
Peptide structure-activity relationship (SAR) analysis: The analog serves as a valuable tool for elucidating the structure-activity relationships within the urotensin peptide family. By systematically substituting amino acids at key positions and assessing resultant changes in biological activity, researchers can pinpoint residues essential for receptor activation and signaling efficacy. Studies involving [Orn5]-URP contribute to a deeper understanding of how side chain modifications influence peptide conformation, receptor engagement, and downstream functional outcomes, advancing the field of peptide-based ligand engineering.
Peptide signaling pathway elucidation: [Orn5]-URP is frequently employed in cellular assays to dissect signaling cascades initiated by UT receptor activation. By comparing the intracellular responses elicited by the analog versus native URP, scientists can distinguish the effects of specific residue modifications on G protein coupling, second messenger generation, and effector pathway activation. Such investigations are instrumental in clarifying the mechanistic basis of urotensinergic signaling and in identifying potential points of pharmacological intervention.
Peptide engineering and design: The incorporation of ornithine into the URP backbone exemplifies a broader strategy in peptide engineering, where non-canonical amino acids are introduced to modulate peptide properties. [Orn5]-URP provides a model for evaluating how unnatural residues affect peptide stability, receptor selectivity, and resistance to proteolytic degradation. Insights gained from these studies inform the rational design of next-generation peptide therapeutics and research probes with enhanced functional profiles.
Analytical method development: The unique sequence and physicochemical characteristics of [Orn5]-URP make it a useful calibrant or reference standard in analytical techniques such as high-performance liquid chromatography (HPLC) and mass spectrometry. Its defined structure allows for precise assay calibration, method validation, and assessment of peptide purity and identity in research workflows focused on synthetic peptide analysis. This utility supports the rigorous characterization and quality control of peptide-based compounds in laboratory settings.
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