Vipivotide tetraxetan Linker is a modular peptide spacer engineered to support conjugation with tetraxetan chelators or targeting motifs. Its sequence balances flexibility with controlled steric bulk to maintain structural accessibility. Researchers evaluate its coordination compatibility and conformational adaptability. Applications include radioligand construction, peptide-chelator engineering, and linker-optimization studies.
CAT No: R2317
CAS No:1703768-74-4
Synonyms/Alias:Vipivotide tetraxetan Linker;1703768-74-4;PSMA-617 Linker;(2S)-2-[[(1S)-5-[[(2S)-2-[[4-(aminomethyl)cyclohexanecarbonyl]amino]-3-naphthalen-2-ylpropanoyl]amino]-1-carboxypentyl]carbamoylamino]pentanedioic acid;JUN68744;PSMA-617 Linker?;(2S)-2-({[(1S)-1-carboxy-5-[(2S)-3-(naphthalen-2-yl)-2-{[(1r,4r)-4-(aminomethyl)cyclohexyl]formamido}propanamido]pentyl]carbamoyl}amino)pentanedioic acid;EX-A9930;AKOS040742816;DA-68599;HY-43869;CS-0095890;F82404;
Vipivotide tetraxetan Linker is a synthetic peptide-based bifunctional chelator designed for advanced applications in radiopharmaceutical development and targeted molecular conjugation. Structurally, it incorporates a DOTA-derived macrocyclic chelator core with a penta-peptidic framework, enabling the stable coordination of radiometals while providing functional groups for site-specific attachment to biomolecules. Its unique architecture facilitates the conjugation of radionuclides to peptides, antibodies, or other targeting vectors, making it highly relevant for research in molecular imaging, targeted delivery, and the creation of novel diagnostic and analytical tools. As a specialized linker, vipivotide tetraxetan serves as a versatile intermediary in the synthesis of complex bioconjugates, supporting innovative approaches in chemical biology and molecular probe design.
Radiolabeling and Chelation: In radiopharmaceutical research, vipivotide tetraxetan's macrocyclic DOTA moiety is widely utilized for its high-affinity chelation of trivalent radiometals such as lutetium-177, yttrium-90, and gallium-68. By forming exceptionally stable complexes, it minimizes metal dissociation and ensures reliable delivery of radioisotopes to intended molecular targets. This property is fundamental in the synthesis of radiolabeled peptides, antibodies, or small molecules for use in preclinical imaging and biodistribution studies, as well as in the development of new radiotracers for positron emission tomography (PET) and single-photon emission computed tomography (SPECT) research.
Bioconjugation and Targeted Delivery: The peptide backbone of vipivotide tetraxetan Linker is engineered with functional groups that allow for site-selective conjugation to a wide range of biomolecules, including peptides, proteins, and antibodies. This facilitates the creation of targeted molecular probes or delivery systems, enabling researchers to couple radionuclides or other payloads to ligands that recognize specific cellular receptors or tissues. Its modular design supports the generation of homogeneous and reproducible conjugates, a critical requirement for mechanistic studies in targeted drug delivery, receptor mapping, and molecular interaction analyses.
Peptide Synthesis and Modification: As a peptide-based linker, vipivotide tetraxetan is frequently employed in solid-phase peptide synthesis (SPPS) protocols to introduce chelating functionality into custom peptide sequences. The incorporation of this linker during synthesis enables downstream radiolabeling or metal complexation without compromising the integrity or bioactivity of the parent peptide. This approach is particularly valuable in the design of multifunctional peptides for research into receptor targeting, biomarker validation, or the development of molecular imaging agents.
Analytical and Bioanalytical Applications: The robust metal-chelating capabilities of vipivotide tetraxetan Linker also make it suitable for use in analytical workflows requiring precise quantification or detection of biomolecules. By facilitating the attachment of radiometals or stable isotopes to peptides and proteins, it enhances the sensitivity and specificity of mass spectrometry, radioimmunoassays, and related bioanalytical techniques. Researchers leverage these properties to track molecular interactions, study pharmacokinetics, or validate biomarker expression in complex biological samples.
Structure-Activity Relationship (SAR) Studies: In the context of chemical biology and medicinal chemistry, vipivotide tetraxetan Linker is instrumental in the systematic evaluation of structure-activity relationships. Its ability to introduce radiolabels or metal tags into defined sites of peptides or proteins allows for the precise mapping of binding domains, the assessment of ligand-receptor interactions, and the optimization of targeting vectors. These studies provide critical insights for the rational design of next-generation molecular probes, imaging agents, and targeted synthetic constructs for research applications.
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