Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor drug candidate. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of streptozotocin (STZ)-induced diabetes. Cenupatide was found to revert STZ-induced up-regulation of uPA levels and activity, while uPAR on podocytes and (s)uPAR were unaffected. In glomeruli, Cenupatide inhibited FPR2 expression suggesting that the drug may act downstream uPAR, and recovered the increased activity of the αvβ3 integrin/Rac-1 pathway indicating a major role of uPAR in regulating podocyte function.
CAT No: R1917
CAS No:1006388-38-0
Synonyms/Alias:Cenupatide;Cenupatide [INN];A92EH9EGL4;UNII-A92EH9EGL4;1006388-38-0;L-PHENYLALANINAMIDE, N2-ACETYL-L-ARGINYL-2-METHYLALANYL-L-ARGINYL-.ALPHA.-METHYL-;L-Phenylalaninamide, N2-acetyl-L-arginyl-2-methylalanyl-L-arginyl-alpha-methyl-;cenupatida;cenupatidum;HY-P1615;DA-51772;CS-0062771;(2S)-2-acetamido-N-[1-[[(2S)-1-[[(2S)-1-amino-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamide;
Chemical Name:(2S)-2-acetamido-N-[1-[[(2S)-1-[[(2S)-1-amino-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]-5-(diaminomethylideneamino)pentanamide
Cenupatide is a synthetic peptide compound designed to mimic and modulate specific biological activities relevant to metabolic and endocrinological research. Structurally, it belongs to the class of glucagon-like peptide-1 (GLP-1) receptor agonists, a group of peptides that play a pivotal role in the regulation of glucose homeostasis and appetite signaling pathways. Its engineered sequence and stability enhancements make it a valuable tool for probing peptide-receptor interactions, studying peptide pharmacodynamics, and developing next-generation peptide-based research tools. Researchers utilize this compound to explore the intricate mechanisms of peptide hormone action and to advance understanding in fields such as metabolic regulation, signal transduction, and peptide therapeutics discovery.
Peptide-receptor interaction studies: Cenupatide serves as a robust model system for investigating the molecular dynamics of GLP-1 receptor engagement. By employing it in receptor binding assays, researchers can delineate the structural features and critical residues responsible for high-affinity binding and receptor activation. These studies contribute to a deeper understanding of peptide-receptor specificity, allosteric modulation, and downstream signaling cascades, supporting the rational design of novel peptide ligands with tailored pharmacological profiles.
Metabolic pathway research: The peptide's activity profile makes it an essential reagent for elucidating the regulatory networks governing glucose metabolism and energy balance. In vitro and ex vivo experimental systems benefit from its use in dissecting the signaling pathways activated by GLP-1 receptor stimulation, including cAMP production, insulinotropic effects, and modulation of cellular nutrient sensing. Such research is foundational for mapping the biochemical landscape of metabolic disorders and for identifying potential intervention points within metabolic signaling pathways.
Peptide stability and pharmacokinetic analysis: Due to its engineered sequence and improved resistance to enzymatic degradation, cenupatide is frequently utilized in studies focused on peptide stability and pharmacokinetics. Researchers can employ the compound in plasma stability assays or simulated gastrointestinal environments to evaluate degradation kinetics, metabolic half-life, and bioavailability. Insights gained from these experiments inform the development of more stable peptide analogues and optimize delivery strategies for peptide-based agents in research settings.
High-throughput screening and assay development: The defined biological activity and receptor selectivity of cenupatide enable its use as a reference standard or positive control in high-throughput screening assays. Scientists leverage its properties to validate assay performance, compare the efficacy of novel peptide candidates, and refine screening protocols targeting GLP-1 receptor-mediated pathways. Such applications accelerate the identification and optimization of new research peptides with desired functional attributes.
Peptide synthesis and structure-activity relationship (SAR) studies: Cenupatide also finds utility as a template for peptide synthesis and SAR investigations. By introducing systematic modifications to its amino acid sequence, researchers can probe the relationship between structure and biological activity, identify critical motifs for receptor engagement, and engineer analogues with enhanced selectivity or stability. These efforts are instrumental in advancing peptide chemistry and in expanding the toolkit available for peptide-based research applications.
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