Angiopep-2 contains a balanced hydrophobic-polar motif supporting transport and receptor-mediated uptake studies. The sequence aids examination of peptide translocation, structural adaptability, and binding determinants. Researchers apply it in molecular trafficking and membrane-interaction research. Its defined architecture supports advanced biochemical characterization.
CAT No: PI-002
Chemical Name:(2S,5S,8S,14S,17S,20S,23S,26S,29S,35S,38S,47S,50S,53S,57R)-56-amino-20,23-bis(2-amino-2-oxoethyl)-14,29-bis(4-aminobutyl)-17,50,53-tribenzyl-5,8-bis(2-carboxyethyl)-26,35-bis(3-guanidinopropyl)-57-hydroxy-2,47-bis(4-hydroxybenzyl)-11-((R)-1-hydroxyethyl)-38-(hydroxymethyl)-4,7,10,13,16,19,22,25,28,31,34,37,40,43,46,49,52,55-octadecaoxo-3,6,9,12,15,18,21,24,27,30,33,36,39,42,45,48,51,54-octadecaazaoctapentacontanoic acid
Angiopep-2 is a synthetic peptide derived from the Kunitz domain of aprotinin, recognized for its unique ability to facilitate transcytosis across the blood-brain barrier (BBB) via low-density lipoprotein receptor-related protein-1 (LRP1)-mediated transport. As a member of the peptide compound category, Angiopep-2 has garnered significant attention in biochemical research due to its exceptional capacity to enhance central nervous system (CNS) delivery of various molecular cargos. Its well-characterized sequence and functional properties make it a valuable tool for investigating peptide-mediated transport mechanisms, optimizing drug delivery strategies, and advancing neuropharmaceutical research.
Blood-Brain Barrier Transport Studies: Angiopep-2 is widely utilized in in vitro and in vivo models to elucidate the mechanisms underlying receptor-mediated transcytosis across the BBB. By conjugating this peptide to various probes or nanoparticles, researchers can quantitatively assess its efficiency in facilitating CNS penetration relative to other transport motifs. Such studies provide critical insights into the molecular determinants of BBB permeability and contribute to the rational design of next-generation delivery vectors for neurological research applications.
Targeted Delivery Vector Development: The peptide serves as a robust targeting ligand in the development of delivery systems aimed at the CNS. Its high affinity for LRP1 allows for selective transport of conjugated molecules, such as imaging agents, nucleic acids, or therapeutic analogs, into brain parenchyma. Incorporation of Angiopep-2 into nanoparticles, liposomes, or polymeric carriers enables the evaluation of targeted delivery efficiency, biodistribution, and uptake mechanisms, thereby supporting the advancement of brain-targeted research tools.
Peptide-Cargo Conjugate Optimization: Angiopep-2 is instrumental in the synthesis and functional assessment of peptide-cargo conjugates. Researchers employ it as a modular linker to attach diverse bioactive molecules, facilitating studies on how peptide architecture, cargo size, and linker chemistry influence transport efficiency and biological activity. Such work is essential for optimizing the design of multifunctional conjugates intended for CNS research and for dissecting the structure-activity relationships governing peptide-mediated delivery.
Neuropharmacokinetic Profiling: The peptide is frequently used in neuropharmacokinetic studies to characterize the distribution, retention, and clearance of CNS-targeted agents. By labeling or conjugating compounds with Angiopep-2, investigators can monitor the temporal and spatial dynamics of brain uptake in both cellular and animal models. These studies are pivotal for understanding the pharmacokinetic behaviors of novel CNS research agents and for comparing the relative performance of different targeting strategies.
Receptor-Ligand Interaction Analysis: Angiopep-2 provides a valuable platform for probing the interactions between peptides and LRP1 or related receptors. Its well-defined binding characteristics enable detailed studies of receptor specificity, binding kinetics, and competitive inhibition, which are fundamental for elucidating the molecular basis of receptor-mediated endocytosis and transcytosis. Such analyses inform both basic research in receptor biology and the applied development of receptor-targeted delivery systems for neurobiological studies.
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