Difelikefalin is a novel and potent kappa-opioid receptor agonist, exhibits low P450 CYP inhibition and low penetration into the brain. Difelikefalin may be useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.
CAT No: R1893
CAS No:1024828-77-0
Synonyms/Alias:Difelikefalin;1024828-77-0;CR845;CR-845;MR13A9;Difelikefalin [INN];difelicefalina;difelikefaline;Difelikefalin (CR845);FE202845;UNII-NA1U919MRO;NA1U919MRO;FE-202845;MR-13A9;CR 845;SEQ ID NO: 2;1024828-77-0 (free base);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;4-Piperidinecarboxylic acid, N1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-;4-Piperidinecarboxylic acid, 4-amino-1-((2R)-6-amino-2-(((2R)-2-(((2R)-2-(((2R)-2-amino-1-oxo-3-phenylpropyl)amino)-1-oxo-3-phenylpropyl)amino)-4-methyl-1-oxopentyl)amino)-1-oxohexyl)-;1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-aminopiperidine-4-carboxylic acid;4-AMINO-1-(D-PHENYLALANYL-D-PHENYLALANYL-D-LEUCYL-D-LYSYL)PIPERIDINE-4-CARBOXYLIC ACID;4-Piperidinecarboylic acid, 4-amino-1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-;N-((2R)-1-(((2R)-1-(((2R)-6-Amino-1-(4-amino-4-carboxy-1-piperidinyl)-1-oxo-2-hexanyl)amino)-4-methyl-1-oxo-2-pentanyl)amino)-1-oxo-3-phenyl-2-propanyl)-D-phenylalaninamide;difelikefalinum;Kapruvia;D-Phe-D-Phe-D-Leu-D-Lys-(gamma-(4-N-piperidinyl)amino carboxylic acid);D-Phe-D-Phe-D-Leu-D-Lys-[gamma-(4-N-piperidinyl)amino carboxylic acid];Difelikefalin TFA;Difelikefalin (USAN/INN);Difelikefalin [USAN:INN];DIFELIKEFALIN [USAN];DIFELIKEFALIN [WHO-DD];GTPL9044;CHEMBL3989915;SCHEMBL10316464;BDBM235785;DTXSID401032896;DIFELIKEFALIN ACETATE [JAN];BCP24752;EX-A5855;AKOS040756421;AT30197;DB11938;BD177570;DA-52529;HY-17609;MS-31091;CR-845; FE-202845;CS-0014687;NS00072889;D11111;US9359399, 2;EN300-7445060;Q21098992;4-amino-1-[(2R)-6-amino-2-[(2R)-2-[(2R)-2-[(2R)-2-amino-3-phenylpropanamido]-3-phenylpropanamido]-4-methylpentanamido]hexanoyl]piperidine-4-carboxylic acid;Difelikefalin; 4-Piperidinecarboxylic acid, N1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-; N1-(D-Phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-4-piperidinecarboxylic acid; CR 845; Difelikefalin;
Chemical Name: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
Difelikefalin is a synthetic peptide compound that functions as a selective agonist of the kappa-opioid receptor (KOR), exhibiting high affinity and specificity for peripheral KORs while demonstrating minimal central nervous system penetration. As a peptide, it is structurally engineered to optimize receptor selectivity and metabolic stability, making it a valuable tool in neuropharmacological and receptor biology research. Its unique pharmacological profile has positioned it as a subject of significant interest in studies focused on peripheral opioid signaling, pain modulation, and the development of next-generation peptide therapeutics. The compound's well-defined receptor activity and peptide backbone support a range of experimental and analytical applications within biochemical and pharmacological research domains.
Receptor Pharmacology Research: Difelikefalin is widely utilized in the characterization of kappa-opioid receptor function, particularly in peripheral tissues. Its high selectivity allows researchers to dissect KOR-mediated signaling pathways without significant interference from mu- or delta-opioid receptors. By applying this peptide in receptor binding assays, signal transduction studies, and functional assays, investigators can elucidate the molecular mechanisms underlying KOR activation, downstream effector engagement, and receptor desensitization or internalization dynamics.
Peptide Structure-Activity Relationship (SAR) Studies: The compound serves as a reference molecule for examining the impact of structural modifications on KOR selectivity, potency, and metabolic stability in peptide ligands. Researchers employ difelikefalin as a benchmark in SAR investigations to compare novel analogs or derivatives, thereby enabling rational design and optimization of new peptide-based KOR agonists. Such studies contribute to a deeper understanding of the structural determinants governing receptor interaction and functional outcomes.
Peripheral Opioid System Investigation: Due to its restricted central nervous system penetration, difelikefalin is particularly valuable in studies targeting the peripheral opioid system. It provides a model for evaluating peripheral receptor-mediated biological responses, such as modulation of nociceptive signaling, pruritus pathways, or inflammatory processes. Researchers leverage its pharmacokinetic and pharmacodynamic properties to differentiate peripheral from central opioid effects in both in vitro and ex vivo experimental systems.
Analytical Method Development: The distinct physicochemical and pharmacological characteristics of difelikefalin make it an appropriate standard or reference compound in the development and validation of analytical methodologies. Techniques such as liquid chromatography-mass spectrometry (LC-MS), high-performance liquid chromatography (HPLC), and receptor-ligand binding assays benefit from its defined properties, supporting accurate quantification, stability assessment, and detection of peptide-based KOR agonists in complex biological matrices.
Peptide Synthesis and Degradation Studies: As a synthetic peptide with established bioactivity, difelikefalin is frequently employed in investigations of peptide synthesis methodologies and metabolic degradation pathways. Its use enables researchers to evaluate the efficiency of synthetic strategies, monitor peptide stability under various experimental conditions, and characterize enzymatic degradation products. These studies inform the development of robust synthetic protocols and contribute to the broader understanding of peptide pharmacokinetics and biotransformation.
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