Edotreotide is a chelated octreotide derivative with somatostatin activity. Edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of octreotide and chelated via dodecanetetraacetic acid (DOTA). Like octreotide, this edotreotide binds to somatostatin receptors (SSTRs), especially type 2, present on the cell membrane of many types of neuroendocrine tumors.
CAT No: 10-101-210
CAS No:204318-14-9
Synonyms/Alias:DOTA-[TYR3]-OCTREOTIDE;DOTATOC;DOTA-FCYWKTCT-OL (DISULFIDE BRIDGE: 2-7);DOTA-D-PHE-CYS-TYR-D-TRP-LYS-THR-CYS-THR-OL (DISULFIDE BRIDGE: 2-7);[DOTA-DPHE1, TYR3]OCTREOTIDE;DOTA-D-PHE-CYS-TYR-D-TRP-LYS-THR-CYS-THREONINOL;EDOTREOTIDE;4,7,10-TRICARBOXYMETHYL-1,4,7,10-TETRAAZA-CYCLODODECAN-1-YL-ACETYL-D-PHE-CYS-TYR-D-TRP-LYS-THR-CYS-L-THREONINOL, (DISULFIDE BOND)
Edotreotide, also known as [DOTA0,Tyr3]octreotide or DOTATOC, is a synthetic somatostatin analog conjugated with the chelator DOTA, designed for high-affinity binding to somatostatin receptors, particularly subtype 2. As a carbohydrate-based peptide compound, Edotreotide combines the targeting capabilities of octreotide with the versatile radiolabeling functionality of DOTA, enabling its use in a variety of advanced research and diagnostic applications. Its unique structure allows for stable complexation with a range of radiometals, facilitating sensitive and specific localization of somatostatin receptor-expressing cells in biological systems. The molecule's robust receptor affinity and chemical stability have made it a valuable tool in preclinical and translational research, particularly in studies involving neuroendocrine cell biology and molecular imaging. Its versatility has positioned it at the forefront of innovations in receptor-targeted imaging and radiopharmaceutical development.
Receptor Targeting Studies: Edotreotide is widely utilized in receptor targeting studies due to its high specificity for somatostatin receptor subtype 2. Researchers employ it to investigate receptor expression patterns in various cell lines and tissue samples, using radiolabeled versions to quantitatively assess binding kinetics and receptor density. These studies provide critical insights into the distribution and functional roles of somatostatin receptors in both normal and pathological conditions, supporting the development of novel diagnostic and therapeutic strategies.
Molecular Imaging Research: In molecular imaging research, DOTATOC serves as an essential probe for visualizing somatostatin receptor-positive tissues in animal models. By labeling it with gamma- or positron-emitting isotopes, investigators can perform in vivo imaging using modalities such as PET or SPECT. This approach enables noninvasive monitoring of receptor dynamics, tumor localization, and response to experimental interventions, greatly enhancing the understanding of disease progression and therapeutic efficacy at the molecular level.
Radiopharmaceutical Development: The DOTA moiety in Edotreotide allows for the stable chelation of a variety of radiometals, making it a key component in the development of novel radiopharmaceuticals. Researchers leverage this property to create targeted radiotracers for imaging or experimental therapy, optimizing chelation protocols and evaluating the pharmacokinetics and biodistribution of new compounds. These efforts drive innovation in the design of next-generation agents for research in nuclear medicine and molecular diagnostics.
Biodistribution and Pharmacokinetic Studies: Scientists use DOTATOC in biodistribution and pharmacokinetic studies to evaluate how somatostatin analogs distribute, metabolize, and clear in animal models. By tracking radiolabeled Edotreotide, researchers can quantify tissue uptake, retention times, and elimination pathways. Such data inform the optimization of dosing regimens and the improvement of compound design for future research applications, ensuring that new analogs achieve desired targeting and clearance profiles.
Tumor Biology Investigation: Edotreotide is instrumental in investigating the biology of neuroendocrine and other somatostatin receptor-expressing tumors. It enables detailed studies of receptor-mediated signaling, tumor microenvironment interactions, and the effects of receptor modulation in vitro and in vivo. Researchers use it to dissect the molecular mechanisms underlying tumor growth, receptor regulation, and potential resistance pathways, contributing to a deeper understanding of tumor biology and the identification of new research targets.
In summary, Edotreotide stands as a multifaceted research compound, facilitating advancements across receptor targeting, molecular imaging, radiopharmaceutical development, biodistribution studies, and tumor biology investigations. Its combination of high receptor affinity, radiolabeling versatility, and chemical stability ensures its continued relevance in cutting-edge scientific research, supporting the exploration of somatostatin receptor pathways and the development of innovative diagnostic and investigational tools.
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