Difelikefalin ,also known as D-Phe-D-Phe-D-Leu-D-Lys-[γ-(4-N-piperidinyl)amino carboxylic acid] (as the acetate salt), is an analgesic opioid peptide acting as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR).
CAT No: 10-101-174
CAS No:1024828-77-0(net);1024829-44-4
Synonyms/Alias:Difelikefalin acetate;CR845 acetate;CR-845 acetate;1024829-44-4;UNII-0P70AR5BYB;0P70AR5BYB;Korsuva;4-Amino-1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysl)-piperidine-4-carboxylic acid, acetate salt;acetic acid;4-amino-1-[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid;CHEMBL5315123;1024828-77-0 , Difelikefalin;DIFELIKEFALIN ACETATE [WHO-DD];TS-10624;DIFELIKEFALIN ACETATE [ORANGE BOOK];4-Amino-1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)piperidine-4-carboxylic acid acetate;N1-(D-Phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-4-piperidinecarboxylic acid acetate (1:);N1-(D-Phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-4-piperidinecarboxylic acid acetate (1:?);
Difelikefalin acetate is a synthetic peptide compound classified as a selective kappa opioid receptor (KOR) agonist. Structurally engineered to interact primarily with peripheral KORs, it is distinguished by its peptide backbone and high receptor selectivity, making it a prominent tool in the study of opioid pharmacology and signal transduction. Owing to its hydrophilic nature and limited blood-brain barrier penetration, difelikefalin acetate is particularly valuable for dissecting peripheral versus central opioid receptor functions. Its unique pharmacodynamic profile has established it as an important agent in research settings focused on pain modulation, receptor-ligand interactions, and the development of novel opioid-based probes.
Receptor pharmacology studies: Difelikefalin acetate serves as a precise probe for investigating kappa opioid receptor signaling pathways. Researchers utilize this peptide to characterize receptor activation, downstream G-protein coupling, and β-arrestin recruitment in in vitro systems. Its selectivity enables the differentiation of KOR-mediated responses from those of mu and delta opioid receptors, facilitating the elucidation of receptor subtype-specific mechanisms. This specificity is particularly useful in studies aiming to map the physiological roles of KORs in various tissues, including neural and peripheral cell types.
Peptide structure-activity relationship (SAR) analysis: As a synthetic peptide with well-defined modifications, difelikefalin acetate is frequently employed in SAR studies to explore how structural changes influence receptor affinity, efficacy, and selectivity. By serving as a reference compound, it aids in the rational design and optimization of new peptide-based KOR agonists. Such SAR investigations are essential for advancing the understanding of the molecular determinants governing receptor-ligand interactions and for guiding the synthesis of next-generation opioid peptides with improved pharmacological properties.
Peripheral opioid research: The limited central nervous system penetration of difelikefalin acetate makes it an ideal tool for distinguishing peripheral from central opioid effects. Scientists leverage its pharmacokinetic profile to study the modulation of pain and inflammatory pathways mediated by peripheral KORs without confounding central side effects. This application is particularly relevant in research models that aim to dissect the roles of peripheral opioid receptors in nociception, pruritus, and gastrointestinal physiology.
In vitro assay development: Difelikefalin acetate is widely used as a standard agonist in the development and validation of cell-based assays targeting kappa opioid receptors. Its predictable and reproducible pharmacological activity supports the calibration of high-throughput screening platforms, receptor binding assays, and functional bioassays. These systems are critical for drug discovery programs focused on identifying new KOR modulators and for quality control in peptide research laboratories.
Peptide stability and metabolism studies: The compound's peptide nature and defined sequence make it a suitable model for investigating peptide stability, degradation pathways, and metabolic fate in biological matrices. Researchers employ difelikefalin acetate to evaluate enzymatic cleavage, peptide half-life, and the influence of chemical modifications on metabolic resistance. Insights gained from such studies contribute to the broader field of peptide drug development, informing strategies to enhance peptide stability and bioavailability in experimental systems.
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