PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.
CAT No: R1810
CAS No:352017-71-1
Synonyms/Alias:352017-71-1;AY-NH2;H-Ala-Tyr-Pro-Gly-Lys-Phe-NH2;PAR-4 Agonist Peptide, amide;(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)-2-[[(2S)-2-aminopropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxamide;PAR-4-AP;AY-NH2;PAR-4-AP;AY-NH2?;HY-P1309;AKOS024456631;NCGC00485629-01;DA-69120;CS-0029355;G13369;(Ala1)-PAR-4 (1-6) amide (mouse) trifluoroacetate salt;
PAR-4 Agonist Peptide, amide is a synthetic peptide designed to selectively activate protease-activated receptor-4 (PAR-4), a member of the G-protein coupled receptor family involved in diverse cellular signaling pathways. As a biochemically defined agonist, it enables precise modulation of PAR-4-mediated processes, making it a valuable tool for dissecting the physiological and molecular roles of this receptor. The amide modification at the C-terminus enhances its resistance to enzymatic degradation, ensuring greater stability and reproducibility in experimental systems. Its defined sequence and functional specificity have positioned it as a key reagent in studies of signal transduction, platelet biology, and vascular research.
Receptor signaling studies: In cell-based assays and in vitro systems, PAR-4 Agonist Peptide, amide is widely used to activate PAR-4 and study the downstream signaling cascades initiated by this receptor. By selectively triggering PAR-4, researchers can delineate its unique contributions to intracellular pathways such as calcium mobilization, MAPK activation, and phosphoinositide turnover. This targeted activation is essential for distinguishing PAR-4-specific responses from those mediated by other protease-activated receptors, thereby enabling detailed mechanistic investigations of receptor function and regulation.
Platelet function research: The peptide serves as a robust tool for probing platelet activation mechanisms, as PAR-4 is a critical mediator of thrombin-induced platelet aggregation. Utilizing this agonist, investigators can induce platelet responses in isolated platelet-rich plasma or washed platelet preparations, allowing for the assessment of aggregation, granule release, and integrin activation independent of thrombin's pleiotropic effects. These studies are fundamental for understanding the molecular basis of hemostasis, thrombosis, and platelet-related vascular disorders.
Vascular biology and endothelial studies: PAR-4 Agonist Peptide, amide provides a controlled means of activating PAR-4 in endothelial cells and vascular smooth muscle cells, enabling researchers to explore its role in vascular tone regulation, permeability, and inflammatory signaling. Through selective stimulation, the peptide facilitates experiments investigating the interplay between PAR-4 activation and endothelial barrier function, cytokine release, or cell adhesion molecule expression, offering insights into vascular homeostasis and pathology.
Drug discovery and pharmacological profiling: In the context of drug screening and pharmacological research, the peptide is instrumental for characterizing the efficacy and specificity of novel PAR-4 antagonists or modulators. By serving as a reference agonist, it allows for the quantitative evaluation of candidate compounds' inhibitory effects on PAR-4-mediated responses, supporting lead optimization and structure-activity relationship studies. This application is particularly relevant for the development of targeted therapies addressing thrombotic or inflammatory conditions in preclinical models.
Peptide structure-activity relationship analyses: The defined sequence and functional activity of PAR-4 Agonist Peptide, amide make it a valuable standard in structure-activity relationship (SAR) investigations. Researchers employ the peptide to compare the biological effects of sequence analogs, truncated variants, or modified peptides, thereby elucidating the structural determinants of PAR-4 activation. These SAR studies inform the rational design of next-generation agonists or antagonists with improved selectivity and potency, advancing the field of peptide-based research and therapeutic innovation.
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