Angiopep-2 TFA contains hydrophobic and polar residues arranged to promote receptor interaction and peptide trafficking studies. The sequence assists in modeling membrane affinity, structural adaptability, and ligand-binding properties. Researchers employ it in conformational and biophysical analyses. Its TFA salt improves handling and solubility.
CAT No: R2229
CAS No:906480-05-5
Synonyms/Alias:Angiopep-2 TFA;906480-05-5;SCHEMBL22807671;
Angiopep-2 TFA is a synthetic peptide derived from the Kunitz domain of aprotinin, widely recognized for its ability to facilitate transcytosis across the blood-brain barrier (BBB). As a member of the angiopep family, this compound features a unique amino acid sequence that enables high-affinity interaction with low-density lipoprotein receptor-related protein-1 (LRP1), a key mediator of transport processes in the central nervous system. Its trifluoroacetate (TFA) salt form enhances stability and solubility, making it particularly amenable for laboratory handling and formulation. Angiopep-2 TFA has emerged as a powerful research tool for investigating brain-targeted delivery strategies, neuropharmacology, and receptor-mediated transport mechanisms, thus holding significant value for advanced biochemical and pharmaceutical research.
Blood-Brain Barrier Transport Studies: Angiopep-2 TFA is extensively utilized in the study of receptor-mediated transcytosis across the BBB. Its high specificity for LRP1 allows researchers to model and quantify peptide transport dynamics in in vitro and in vivo systems. By serving as a molecular probe, the peptide aids in elucidating the mechanisms underlying selective permeability of the BBB, advancing understanding of how macromolecules traverse this tightly regulated interface.
Drug Delivery Research: In the context of targeted delivery, Angiopep-2 TFA is frequently conjugated to nanoparticles, proteins, or other therapeutic agents to evaluate their capacity for enhanced brain uptake. Its well-characterized interaction with LRP1 makes it a preferred ligand for the design of brain-penetrant delivery vehicles. Researchers employ it to assess the efficiency, specificity, and kinetics of novel carrier systems, thereby supporting the development of next-generation central nervous system delivery platforms.
Receptor-Ligand Interaction Analysis: The peptide's affinity for LRP1 also makes it an ideal tool for studying receptor-ligand interactions at the molecular and cellular levels. Using biophysical and biochemical assays, scientists can investigate binding kinetics, receptor expression, and downstream signaling events. These studies contribute to a deeper understanding of LRP1's physiological roles and its potential as a target for modulating BBB transport.
Peptide Engineering and Optimization: Angiopep-2 TFA serves as a reference sequence in the rational design and optimization of BBB-penetrant peptides. Comparative studies involving analogues or sequence modifications leverage its established activity profile to identify structural features critical for receptor recognition and transport efficiency. Such research underpins the iterative development of improved peptide vectors for brain-targeted applications.
In vivo Imaging and Tracer Development: The unique transport properties of Angiopep-2 TFA have prompted its use in the development of imaging agents and molecular tracers for brain research. By labeling the peptide with fluorescent dyes or radiotracers, researchers can visualize and quantify its biodistribution, brain accumulation, and clearance in animal models. These applications are instrumental for validating delivery strategies and mapping peptide transport pathways within the central nervous system.
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