FC131 TFA is a cyclic peptide analog featuring rigidifying constraints and a mix of aromatic and basic residues. The scaffold supports studies of ligand conformation, metal coordination, and hydrophobic interactions. Researchers use it to analyze structural determinants of peptide binding. Its TFA salt enhances solubility for analytical assays.
CAT No: R2222
CAS No:842166-42-1
Synonyms/Alias:FC131 TFA;FC131 (TFA);842166-42-1;FC131 TFA (606968-52-9 free base);CHEMBL2180076;HY-P1104A;EX-A11276;AKOS040763979;MS-31562;CS-0098047;G17249;2-[3-[(2S,5S,8S,14R)-5-[3-(diaminomethylideneamino)propyl]-14-[(4-hydroxyphenyl)methyl]-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]propyl]guanidine;2,2,2-trifluoroacetic acid;N-{3-[(2S,5S,8S,14R)-5-(3-carbamimidamidopropyl)-14-[(4-hydroxyphenyl)methyl]-8-(naphthalen-2-ylmethyl)-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]propyl}guanidine; trifluoroacetic acid;
FC131 Tfa is a synthetic peptide compound recognized for its potent and selective antagonism of the chemokine receptor CXCR4. As a cyclic peptide derivative, it exhibits high affinity for CXCR4, making it an important molecular tool in the study of chemokine-mediated signaling pathways. FC131 Tfa's unique structural features, including its stability and receptor specificity, have positioned it as a valuable research agent for dissecting the physiological and pathological roles of CXCR4 in various cellular contexts. Its use is particularly relevant in investigations of cell migration, immune cell trafficking, and mechanisms of disease progression where CXCR4 is implicated.
Receptor Binding Studies: FC131 Tfa is widely employed in receptor-ligand binding assays to characterize the pharmacological properties of CXCR4. By serving as a reference antagonist, it enables researchers to quantify receptor occupancy, assess binding affinities of novel ligands, and elucidate the structural determinants of CXCR4 interaction. Such studies are fundamental for advancing the understanding of chemokine receptor biology and for the rational design of next-generation modulators targeting this receptor.
Signal Transduction Analysis: The compound is instrumental in probing downstream signaling events triggered by CXCR4 activation. By inhibiting receptor function, FC131 Tfa allows for the dissection of intracellular pathways such as calcium mobilization, MAP kinase activation, and gene transcription events that are initiated upon chemokine binding. These investigations provide critical insights into the molecular mechanisms governing cell behavior and contribute to the broader field of signal transduction research.
Cell Migration and Chemotaxis Assays: FC131 Tfa is routinely utilized in in vitro models to study the role of CXCR4 in cell migration and chemotaxis. By blocking CXCR4-mediated responses, it helps delineate the contribution of this receptor to the directed movement of cells, particularly in immune cell trafficking, stem cell homing, and metastatic processes. The ability to modulate chemokine-driven migration is essential for unraveling the complexities of cellular dynamics in both physiological and pathological settings.
Peptide Structure-Activity Relationship (SAR) Studies: As a well-characterized cyclic peptide antagonist, FC131 Tfa serves as a benchmark molecule in structure-activity relationship investigations. Researchers leverage its defined sequence and functional properties to guide the design, synthesis, and optimization of novel peptide-based CXCR4 modulators. Comparative SAR analyses involving FC131 Tfa facilitate the identification of key structural motifs responsible for receptor binding and antagonistic activity, thus informing the development of improved research tools.
CXCR4 Pathway Validation: In studies aiming to validate the involvement of CXCR4 in specific biological processes, FC131 Tfa provides a robust means of pharmacological intervention. Its use in functional assays enables the selective inhibition of CXCR4, allowing researchers to confirm the receptor's role in cellular responses such as proliferation, adhesion, and survival. This targeted approach is particularly valuable in deciphering the contributions of chemokine signaling to complex biological systems and disease models.
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