A selective proteinase activated receptor-4 (PAR4) antagonist that inhibits endostatin release and platelet aggregation induced by thrombin.
CAT No: R0887
CAS No:327177-34-4
Synonyms/Alias:TCY-NH2;327177-34-4;(trans-Cinnamoyl)-YPGKF-NH2;(2S)-N-[2-[[(2S)-6-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]-1-[(2S)-3-(4-hydroxyphenyl)-2-[[(E)-3-phenylprop-2-enoyl]amino]propanoyl]pyrrolidine-2-carboxamide;YPGKF;SCHEMBL5058350;HY-P1263;AKOS024456632;DA-68010;CS-0029155;
(trans-Cinnamoyl)-YPGKF-NH2 is a synthetic pentapeptide featuring a trans-cinnamoyl group at the N-terminus and an amidated C-terminus, conferring enhanced stability and distinct physicochemical properties. This peptide is structurally related to the YPGKF motif, which is of interest in peptide science due to its sequence resemblance to endogenous opioid peptides and its potential for receptor interaction studies. The cinnamoyl modification further imparts unique conformational rigidity and hydrophobicity, making it a valuable tool for probing structure-activity relationships and for applications in peptide-based research. As a chemically defined peptide, it supports a range of investigations into peptide-receptor interactions, molecular recognition, and bioactive peptide design.
Peptide receptor binding studies: The cinnamoyl-modified YPGKF sequence is frequently utilized in receptor binding assays to elucidate the interaction between synthetic peptides and opioid receptors or related G-protein coupled receptors. Researchers employ this pentapeptide to dissect the influence of N-terminal modifications, such as the trans-cinnamoyl group, on receptor affinity and selectivity, providing insight into the structural determinants of ligand recognition and signaling. Such studies are instrumental in mapping binding sites and understanding the pharmacophoric requirements for receptor activation or inhibition.
Structure-activity relationship analysis: The unique combination of the YPGKF sequence and the trans-cinnamoyl cap makes this peptide a valuable model for structure-activity relationship (SAR) investigations. By comparing its biological and biophysical properties to those of unmodified or differently modified analogs, scientists can systematically assess how specific chemical groups affect peptide conformation, stability, and functional activity. This approach aids in the rational design of novel peptides with tailored properties for research or industrial applications.
Peptide stability and proteolytic resistance testing: The amidated C-terminus and the bulky cinnamoyl modification at the N-terminus enhance the resistance of the pentapeptide to enzymatic degradation. Researchers leverage these features to study the impact of terminal modifications on peptide half-life in various biological or simulated environments. Such investigations inform the development of peptides with improved stability profiles, which is critical for their use in biochemical assays, delivery systems, or as molecular probes.
Analytical method development: The well-defined sequence and chemical modifications of (trans-Cinnamoyl)-YPGKF-NH2 make it an excellent reference standard or test substrate in analytical chemistry. It is employed in the calibration and validation of chromatographic, spectrometric, or mass spectrometric methods designed for peptide detection, quantification, and characterization. These applications are essential for ensuring the accuracy and reproducibility of peptide analysis in research and quality control laboratories.
Peptide-membrane interaction studies: The increased hydrophobicity conferred by the cinnamoyl group enables this pentapeptide to serve as a model compound in studies of peptide-membrane interactions. Researchers use it to investigate how N-terminal aromatic modifications influence peptide insertion, orientation, and dynamics within lipid bilayers or micellar systems. Insights gained from such studies contribute to the understanding of peptide transport, cellular uptake, and the design of membrane-active peptides for research applications.
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