Isotope labelled Pasireotide. Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor®, which is used in the treatment of Cushing's disease.
CAT No: 10-101-197
CAS No:396091-73-9 (non-labelled)
Synonyms/Alias:Cyclo[(2S)-2-phenylglycyl-D-tryptophyl-L-lysyl-O-(phenylmethyl)-L-tyrosyl-L-phenylalanyl-(4R)-4-[[[(2-aminoethyl)amino]carbonyl]oxy]-L-prolyl]-d7; SOM 230-d7SOM 320-d7; Signifor-d7;
Pasireotide-d7 is a deuterated analog of the synthetic cyclic peptide pasireotide, characterized by the incorporation of seven deuterium atoms. As a stable isotope-labeled peptide, it maintains the core structural and functional features of its non-labeled counterpart, making it highly valuable for a range of advanced biochemical and analytical applications. Its unique isotopic signature enables precise differentiation in complex biological matrices, supporting robust quantification and mechanistic studies. The compound's affinity for somatostatin receptors and preserved peptide backbone further enhance its utility in receptor binding assays, pharmacokinetic profiling, and method validation protocols. Researchers leverage this deuterated peptide standard to improve analytical accuracy, investigate metabolic pathways, and facilitate the development of innovative peptide-based methodologies in drug discovery and biochemical research.
Analytical standard in mass spectrometry: Pasireotide-d7 is widely employed as an internal standard in liquid chromatography-mass spectrometry (LC-MS) and tandem mass spectrometry (LC-MS/MS) assays. Its deuterium labeling provides a distinct mass shift, enabling unambiguous identification and quantification of pasireotide and related analogs in biological samples. By closely matching the physicochemical properties of the unlabeled analyte, the deuterated standard corrects for sample preparation variability, matrix effects, and instrumental fluctuations, thereby enhancing the precision and reliability of quantitative bioanalytical methods.
Pharmacokinetic and metabolic studies: In preclinical and in vitro settings, researchers utilize the labeled peptide to elucidate the absorption, distribution, metabolism, and excretion (ADME) profiles of pasireotide. The stable isotope label allows for selective tracking in complex matrices, facilitating the differentiation between exogenous and endogenous or structurally similar peptides. Application of this standard supports accurate measurement of metabolic stability, biotransformation pathways, and metabolite identification, which are critical for understanding peptide pharmacology and optimizing lead candidates in drug development pipelines.
Peptide receptor binding assays: The structural fidelity of pasireotide-d7 to its parent compound makes it suitable for use in receptor binding studies, particularly those targeting somatostatin receptor subtypes. By serving as a reference or tracer in competitive binding experiments, the labeled peptide aids in the determination of binding affinities, receptor selectivity, and ligand-receptor interaction dynamics. This application is essential for characterizing the pharmacological profiles of novel analogs and for validating assay specificity in ligand screening campaigns.
Method development and validation: The incorporation of deuterated standards is a recognized best practice in the development and validation of quantitative analytical methods. Pasireotide-d7 plays a critical role in establishing method accuracy, linearity, sensitivity, and reproducibility for peptide quantification in biological fluids and tissues. Its use supports compliance with rigorous analytical performance criteria, ensuring that developed assays are robust, transferable, and suitable for high-throughput bioanalytical workflows in pharmaceutical and academic laboratories.
Peptide stability and degradation assessments: The deuterium-labeled peptide is also valuable in studies focused on peptide stability, degradation kinetics, and formulation development. By providing a stable and distinguishable reference, it enables researchers to monitor the integrity of pasireotide under various storage, handling, and formulation conditions. Such applications are crucial for optimizing peptide formulation strategies, evaluating shelf life, and ensuring the quality of peptide-based research reagents and investigational compounds.
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