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 is a synthetic peptide inhibitor designed to selectively target the protease-activated receptor-1 (PAR1), a G-protein-coupled receptor implicated in platelet activation and vascular signaling. As a rationally engineered peptide, it functions as a competitive antagonist, blocking thrombin-induced PAR1 signaling without affecting other protease-activated receptors. Its unique mechanism and structural specificity make it a valuable tool for dissecting complex signaling pathways in hemostasis, thrombosis, and vascular biology. Researchers utilize Pz-128 to investigate the molecular underpinnings of platelet function, endothelial responses, and coagulation processes, providing critical insights into cardiovascular and hematological research.
Platelet Function Studies: Pz-128 is widely employed in in vitro and ex vivo assays to delineate the role of PAR1 in platelet activation and aggregation. By selectively inhibiting PAR1-mediated signaling, it enables researchers to distinguish the contributions of this receptor from those of other platelet receptors, such as PAR4 or P2Y12. This application is particularly valuable in studies aiming to unravel the molecular mechanisms of hemostasis, thrombosis, and platelet-mediated vascular inflammation, supporting the development of novel anti-thrombotic strategies and advancing fundamental understanding of platelet biology.
Vascular Biology Research: The peptide inhibitor serves as a critical reagent for probing the effects of PAR1 signaling in endothelial cells and vascular smooth muscle. By blocking PAR1 activation, it allows for the assessment of downstream signaling events, such as calcium mobilization, gene expression changes, and cytoskeletal remodeling. Researchers leverage these properties to investigate endothelial barrier function, vascular permeability, and inflammatory responses, contributing to the elucidation of mechanisms underlying vascular homeostasis and dysfunction.
Signal Transduction Analysis: In cellular and biochemical studies, Pz-128 is used to dissect G-protein-coupled receptor signaling pathways. Its high specificity for PAR1 makes it an indispensable tool for mapping the downstream effectors and molecular interactions triggered by thrombin and related proteases. Application of this peptide in cell-based assays, reporter gene systems, and phosphoproteomic analyses enables detailed characterization of signaling networks, facilitating the identification of novel regulatory nodes and therapeutic targets within the PAR1 axis.
Drug Discovery and Screening: The compound is frequently utilized in high-throughput screening platforms and pharmacological profiling studies to evaluate the efficacy and selectivity of candidate molecules targeting PAR1. Its well-characterized inhibitory profile provides a benchmark for the validation of small molecules, antibodies, or alternative peptide antagonists. By serving as a reference inhibitor, it supports the optimization of lead compounds and the assessment of off-target effects, thereby accelerating the early stages of cardiovascular drug discovery.
Peptide Mechanism-of-Action Studies: As a synthetic peptide, Pz-128 is instrumental in structure-activity relationship (SAR) investigations focused on PAR1 antagonism. Researchers use it to explore the structural determinants of receptor binding, antagonist potency, and selectivity by introducing targeted modifications or analogs. These studies inform the rational design of next-generation peptide inhibitors with improved pharmacological properties, advancing both basic research and translational applications in receptor pharmacology.
4. Low bone turnover and low BMD in Down syndrome: effect of intermittent PTH treatment
5. Implications of ligand-receptor binding kinetics on GLP-1R signalling
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