Pz-128 is a peptide-based inhibitor analog containing aromatic, basic, and hydrophobic residues that shape conformational behavior. The sequence supports investigation of ligand-protein interactions, backbone flexibility, and helix-adjacent structures. Researchers use it for mapping recognition motifs and solvent-influenced folding. Its architecture aids rigorous biophysical analysis.
CAT No: R2255
CAS No:371131-16-7
Synonyms/Alias:PZ-128;371131-16-7;Palmitate-kksralf-NH2;UNII-IYT6MP4NS9;IYT6MP4NS9;PZ128;PZ 128;L-Phenylalaninamide, N2-(1-oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl-;N2-(1-Oxohexadecyl)-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-alanyl-L-leucyl-L-phenylalaninamide;N-[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]hexadecanamide;N-((2S)-6-amino-1-(((2S)-6-amino-1-(((2S)-1-(((2S)-1-(((2S)-1-(((2S)-1-(((2S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)amino)-5-(diaminomethylideneamino)-1-oxopentan-2-yl)amino)-3-hydroxy-1-oxopropan-2-yl)amino)-1-oxohexan-2-yl)amino)-1-oxohexan-2-yl)hexadecanamide;P1pal-7;CHEMBL4297323;GLXC-20877;AKOS040749254;DB11839;MS-31946;HY-107146;CS-0027429;Palmitoyl-Lys-Lys-Ser-Arg-Ala-Leu-Phe-NH2;G17540;Q27280961;N-((2S,5S,8S,11S,14S,17S,20S)-1,24-diamino-17-(4-aminobutyl)-2-benzyl-11-(3-guanidinopropyl)-14-(hydroxymethyl)-5-isobutyl-8-methyl-1,4,7,10,13,16,19-heptaoxo-3,6,9,12,15,18-hexaazatetracosan-20-yl)palmitamide;
Pz-128, also known as a PAR1 pepducin, is a synthetic lipopeptide designed to modulate the activity of protease-activated receptor 1 (PAR1), a G protein-coupled receptor implicated in various cellular signaling pathways. Engineered to penetrate cell membranes and interact with intracellular receptor domains, Pz-128 offers a unique approach to influencing receptor function from within the cell, distinguishing it from conventional extracellular antagonists. Its structural design enables selective targeting, making it a valuable tool for dissecting the roles of PAR1-mediated signaling in diverse biological processes. The compound's versatility and specificity have attracted significant attention in both basic research and translational studies, positioning it as an essential reagent for investigating the intricate mechanisms underlying PAR1-driven responses.
Platelet Function Research: In the context of platelet biology, Pz-128 serves as a potent modulator for studying the regulation of platelet activation and aggregation. By selectively inhibiting PAR1-mediated signaling, researchers can delineate the precise contributions of this receptor to platelet function, facilitating the exploration of thrombotic pathways and the identification of novel antiplatelet targets. The use of this compound allows for controlled experiments that dissect the interplay between platelet activation and vascular injury, providing a deeper understanding of hemostatic balance and thrombosis.
Vascular Biology and Endothelial Function: The application of Pz-128 extends to the investigation of vascular endothelial responses, where PAR1 signaling plays a critical role in modulating barrier function, inflammation, and vascular tone. Scientists utilize this pepducin to unravel the molecular mechanisms by which endothelial cells respond to physiological and pathological stimuli, such as shear stress or inflammatory mediators. By modulating intracellular receptor activity, it aids in clarifying the downstream signaling events that govern endothelial integrity and vascular homeostasis, supporting the development of strategies to address vascular dysfunction.
Signal Transduction Studies: As a research tool, Pz-128 enables detailed analysis of G protein-coupled receptor signaling cascades. Its ability to penetrate the cell and interact with intracellular domains allows for the selective modulation of signaling pathways downstream of PAR1. Researchers employ the compound to investigate the cross-talk between PAR1 and other signaling networks, elucidating the complexities of receptor-mediated cellular communication. This application is particularly valuable for mapping the intricate web of intracellular events that contribute to cell proliferation, migration, and survival in various biological contexts.
Inflammatory Response Modulation: The study of inflammation benefits from the use of Pz-128, given PAR1's involvement in mediating inflammatory cell recruitment and cytokine release. By controlling PAR1 activity, investigators can assess the impact of targeted receptor modulation on leukocyte-endothelial interactions, chemotaxis, and the expression of pro-inflammatory mediators. This approach provides insights into the molecular underpinnings of inflammatory diseases and supports the identification of potential intervention points for controlling excessive or chronic inflammation.
Cancer Research: The exploration of tumor biology and metastasis has also incorporated Pz-128 as a tool for dissecting the role of PAR1 in cancer cell behavior. Researchers leverage its ability to inhibit PAR1-driven signaling to study processes such as tumor cell invasion, angiogenesis, and the metastatic cascade. Through these investigations, the compound contributes to a better understanding of how GPCR-mediated pathways influence the tumor microenvironment and cancer progression, paving the way for the discovery of novel molecular targets in oncology.
In summary, Pz-128 stands out as a multifaceted research reagent with broad applications across platelet function studies, vascular biology, signal transduction analysis, inflammation research, and oncology. Its unique mechanism of action—targeting intracellular receptor domains—provides researchers with a powerful means to selectively modulate PAR1 activity and unravel the complexities of GPCR signaling in health and disease. By facilitating precise experimental control, this compound continues to drive advancements in our understanding of cellular communication and the development of innovative therapeutic strategies.
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