DOTA-(Tyr3)-octreotate can be obtained through preparation of DOTA-containing peptides and radionucleotide complexes as antitumor agents for treating somatostatin postive tumor and metastasized tumors.
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CAT No: R1831
CAS No:177943-89-4
Synonyms/Alias:177943-89-4;DOTA-(Tyr3)-Octreotate acetate;L-Lysine-1,2,3,4,5,6-13C6-N2,N6-15N2, Hydrochloride; (S)-2,6-Diaminohexanoic acid-13C6,15N2 hydrochloride; 13C and 15N Labeled Lys; 13C and 15N Labeled Lysine Hydrochloride; SILAC Amino Acid;;MFCD09039058;EX-A9168;G13545;
DOTA-[Tyr3]-Octreotide Acid is a synthetic peptide conjugate that incorporates the somatostatin analog octreotide, modified at the third amino acid position with tyrosine and functionalized with a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator. This compound is of significant interest in peptide-based research due to its ability to bind somatostatin receptors with high affinity, particularly subtype 2 (SSTR2), and its compatibility with metal chelation strategies. The integration of the DOTA moiety enables site-specific labeling with a range of metal ions, supporting diverse applications in molecular imaging, radiochemistry, and receptor-targeted studies. Its structure exemplifies the convergence of peptide engineering and chelator chemistry, making it a valuable tool for investigating receptor-ligand interactions and developing novel bioconjugates.
Radiolabeling and Molecular Imaging: DOTA-[Tyr3]-Octreotide Acid is extensively used as a precursor for radiolabeling with metallic radionuclides such as gallium-68, indium-111, or lutetium-177. The DOTA chelator provides robust coordination chemistry, facilitating the stable incorporation of radioisotopes. This enables the preparation of radiolabeled tracers for positron emission tomography (PET) or single-photon emission computed tomography (SPECT), supporting noninvasive imaging of somatostatin receptor-expressing tissues in preclinical models. Researchers utilize these properties to study receptor distribution, tumor biology, and pharmacokinetics, advancing the understanding of peptide-receptor dynamics in living systems.
Receptor Binding Studies: The high affinity of the octreotide scaffold for somatostatin receptor subtypes, particularly SSTR2, makes this peptide conjugate a preferred probe in receptor-ligand binding assays. By introducing isotopic or fluorescent labels via the DOTA group, investigators can quantitatively assess binding kinetics, receptor density, and competitive inhibition profiles in cell lines or tissue samples. These studies are essential for characterizing novel ligands, validating receptor expression, and supporting the rational design of targeted peptide therapeutics and diagnostics.
Peptide Synthesis and Bioconjugation: The modular structure of DOTA-[Tyr3]-Octreotide Acid allows it to serve as a versatile intermediate in advanced peptide synthesis and conjugation workflows. Its DOTA functionality supports further modification with metals, fluorophores, or other bioactive moieties, enabling the generation of multifunctional peptide conjugates. Researchers in chemical biology and pharmaceutical development employ such constructs to explore targeted delivery systems, dual-modality imaging agents, and innovative diagnostic platforms, leveraging the robust synthetic accessibility and tunable properties of the molecule.
Pharmacokinetic and Biodistribution Analysis: The unique combination of a somatostatin analog with a chelating agent allows for detailed pharmacokinetic and biodistribution studies in vivo. By radiolabeling or tagging the compound, scientists can monitor its temporal and spatial distribution, clearance rates, and tissue uptake profiles in animal models. These data are crucial for optimizing peptide design, improving targeting efficiency, and minimizing off-target effects in the context of molecular imaging or targeted delivery research.
Analytical Method Development: DOTA-[Tyr3]-Octreotide Acid is also employed as a reference standard or analytical probe in the development and validation of chromatographic and mass spectrometric methods. Its well-defined structure and chelation properties make it suitable for method calibration, sensitivity assessment, and system suitability testing in laboratories specializing in peptide analytics, radiochemistry, or bioanalytical chemistry. By providing a reliable benchmark, it supports the advancement of robust analytical protocols for peptide-based compounds and conjugates.
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