Acetyl-Octreotide features an acetylated N-terminus that modulates peptide stability and receptor-interaction studies. Its cyclic core and diverse side chains support investigations of conformational rigidity in solution. Researchers analyze its folding, hydrophobic packing, and charge distribution. Applications span peptide-structure modeling, ligand optimization, and signaling-pathway research.
CAT No: R2430
CAS No:83795-61-3
Synonyms/Alias:Acetyl-Octreotide;83795-61-3;HY-P5085;DA-60734;CS-0676026;(4R,7S,10S,13R,16S,19R)-19-[[(2R)-2-acetamido-3-phenylpropanoyl]amino]-10-(4-aminobutyl)-16-benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide;
Acetyl-Octreotide is a synthetic octapeptide analog of somatostatin, engineered to mimic and extend the biological activity of the native hormone while offering enhanced metabolic stability. As a member of the peptide compound class, it is distinguished by an N-terminal acetylation that confers increased resistance to enzymatic degradation, thereby prolonging its functional half-life in experimental systems. Acetyl-Octreotide is widely recognized for its high affinity binding to somatostatin receptors, particularly subtypes 2 and 5, making it a valuable tool in the study of receptor-mediated signaling pathways. Its structural and functional properties render it highly relevant for research focused on neuroendocrine regulation, peptide-receptor interactions, and the broader field of peptide-based molecular probes.
Receptor Binding Studies: Acetyl-Octreotide is extensively utilized in the investigation of somatostatin receptor pharmacology, particularly for mapping receptor subtype selectivity and affinity. Its stable peptide backbone and receptor specificity allow researchers to dissect the molecular determinants underlying ligand-receptor interactions. By serving as a model ligand, it aids in characterizing somatostatin receptor distribution, density, and functional responsiveness in various cellular and tissue models, providing critical insight into G-protein coupled receptor (GPCR) signaling mechanisms.
Signal Transduction Research: The compound is instrumental in studies exploring intracellular signaling cascades initiated by somatostatin receptor activation. Its use enables precise modulation of cyclic AMP levels, calcium flux, and downstream effector pathways, facilitating detailed analysis of inhibitory G-protein (Gi/o) mediated processes. Researchers employ Acetyl-Octreotide to elucidate the regulatory circuits controlling hormone secretion, neurotransmitter release, and cellular proliferation, thereby advancing the understanding of neuroendocrine communication.
Peptide Drug Development: As a stable and bioactive somatostatin analog, Acetyl-Octreotide serves as a template for the rational design and optimization of novel peptide therapeutics. Its structure-function relationship provides valuable data for modifying peptide sequences to enhance receptor selectivity, metabolic stability, and pharmacodynamic profiles. Medicinal chemistry programs leverage these insights to develop next-generation analogs with tailored biological properties for research and preclinical applications.
Radiolabeling and Imaging Probe Development: The high receptor affinity and defined structure of Acetyl-Octreotide make it an attractive candidate for conjugation with radiolabels or fluorescent tags. Such labeled derivatives are employed in receptor binding assays, autoradiography, and in vitro imaging studies to visualize and quantify somatostatin receptor expression. These applications support the development of molecular imaging agents and facilitate the non-invasive study of receptor dynamics in experimental models.
Peptide Synthesis and Analytical Validation: Acetyl-Octreotide is frequently used as a reference standard or positive control in peptide synthesis workflows and analytical method development. Its well-characterized sequence and robust physicochemical properties assist in calibrating chromatographic systems, validating mass spectrometric techniques, and benchmarking peptide purity and identity. This role is essential for ensuring the reliability and reproducibility of peptide-focused research and quality control processes within the laboratory setting.
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