Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.
CAT No: R1953
CAS No:199807-35-7
Synonyms/Alias:Cilengitide trifluoroacetate;199807-35-7;Cilengitide TFA;Cilengitide TFA salt;Cilengitide (TFA);2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid;2,2,2-trifluoroacetic acid;NSC 707544;Cilengitidetrifluoroacetate;Cilengitide (TFA salt)?;Cilengitide?trifluoroacetate;C29H41F3N8O9;EMD 121974 (TFA);MFCD22665738;s7077;AKOS032945134;CCG-270388;BS-15883;DA-62313;HY-16143;CS-0006160;C73784;EMD 121974; NSC 707544;2-((2S,5R,8S,11S)-5-Benzyl-11-(3-guanidinopropyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl)acetic acid trifluoroacetate;
Chemical Name:2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid;2,2,2-trifluoroacetic acid
Cilengitide trifluoroacetate is a synthetic cyclic pentapeptide that functions as a potent and selective inhibitor of integrins, particularly those containing the RGD (Arg-Gly-Asp) recognition motif such as αvβ3 and αvβ5. As a member of the peptide compound category, it is structurally engineered to mimic natural ligands of integrin receptors, thereby modulating cell adhesion, migration, and signaling pathways. Its unique biochemical properties have positioned it as a valuable research tool for probing integrin-mediated biological processes and for advancing the understanding of cell-extracellular matrix interactions in various physiological and pathological contexts.
Integrin inhibitor research: Cilengitide trifluoroacetate is widely utilized in studies investigating the molecular mechanisms of integrin function. By selectively blocking integrin-ligand interactions, it enables researchers to dissect the roles of specific integrin subtypes in cell adhesion, migration, and signal transduction. This has proven especially useful in elucidating the contribution of integrins to processes such as angiogenesis, tissue remodeling, and metastasis in cellular and in vitro models.
Angiogenesis assays: The compound serves as a critical reagent in assays designed to evaluate the regulation of new blood vessel formation. Its ability to disrupt integrin-mediated signaling allows for precise modulation of endothelial cell behavior and vessel sprouting in culture systems. Researchers leverage these properties to better understand the molecular underpinnings of angiogenesis and to screen for novel anti-angiogenic agents in preclinical settings.
Cell migration and invasion studies: Cilengitide trifluoroacetate is frequently employed to investigate the dynamics of cell motility and invasive behavior, particularly in cancer research and tissue engineering. By inhibiting integrin activity, it provides a means to assess the dependency of various cell types on extracellular matrix interactions for movement and invasion. This has facilitated insights into metastatic mechanisms and the identification of potential molecular targets for intervention.
Peptide structure-activity relationship (SAR) analysis: Due to its well-defined cyclic peptide structure and integrin selectivity, cilengitide trifluoroacetate is a reference compound in SAR studies aimed at optimizing peptide-based integrin inhibitors. Researchers use it as a benchmark to evaluate the impact of structural modifications on biological activity, binding affinity, and specificity. This contributes to the rational design of next-generation peptides for both research and potential industrial applications.
Biochemical assay development: The robust inhibitory profile and stability of cilengitide trifluoroacetate make it a valuable standard in the development and validation of biochemical assays targeting integrin function. Laboratories incorporate it into assay systems to calibrate response curves, verify assay sensitivity, and ensure reproducibility in high-throughput screening platforms. Its application in assay development supports the advancement of integrin-focused research in both academic and industrial laboratories.
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