Isotope labelled Linaclotide. Linaclotide is a 14-amino acid peptide indicated for the treatment of adults with CC and IBS-C; agonist of guanylate cyclase C
CAT No: 10-101-194
CAS No:851199-59-2 (non-d)
Synonyms/Alias:L-Cysteinyl-L-cysteinyl-L-α-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-d4-L-cysteinyl-L-threonylglycyl-L-cysteinyl-L-tyrosine Cyclic (1→6),(2→10),(5→13)-Tris(disulfide); 11: PN: WO2008151257 SEQID: 55 claimed protein-d4; 13: PN: WO2008151257 SEQID: 57 Claimed Protein-d4; 2074: PN: US20090062207 SEQID: 3 Claimed Protein-d4; 40: PN: WO2010065751 SEQID: 55 Claimed Protein-d4; 42: PN: WO2010065751 SEQID: 57 claimed protein-d4; 55: PN: US20100152118 SEQID: 55 Claimed Protein-d4; 55: PN: WO2011069038 SEQID: 55 Claimed Sequence-d4; 55: PN: WO2012037380 SEQID: 55 Unclaimed Protein-d4; 57: PN: WO2011069038 SEQID: 57 Claimed Sequence-d4; 57: PN: WO2012037380 SEQID: 57 Claimed Protein-d4
Linaclotide D4 is a deuterium-labeled analog of linaclotide, designed to facilitate advanced research in the field of carbohydrate-based peptide therapeutics. As a synthetic guanylate cyclase-C (GC-C) agonist, this compound possesses a unique isotopic signature that makes it particularly valuable for analytical and experimental applications. With its enhanced stability and traceability, Linaclotide D4 serves as a powerful tool for investigating the pharmacokinetics and metabolic pathways of peptide-based drugs. Its distinctive deuterium incorporation allows for precise differentiation from endogenous and exogenous unlabeled counterparts in complex biological matrices, thereby supporting in-depth scientific studies.
Pharmacokinetic Studies: Linaclotide D4 is extensively utilized in pharmacokinetic research to elucidate absorption, distribution, metabolism, and excretion (ADME) profiles. By leveraging its deuterium label, researchers can track the compound with high specificity using mass spectrometry, enabling the accurate quantification of its concentration over time in various biological samples. This approach provides critical insights into the peptide's metabolic fate and assists in optimizing dosing regimens for investigational purposes.
Metabolic Stability Assessment: The deuterated nature of Linaclotide D4 offers a significant advantage in metabolic stability studies. Scientists employ this compound to compare its resistance to enzymatic degradation relative to non-deuterated linaclotide. Such investigations are crucial for understanding how minor structural modifications, such as deuterium substitution, can influence peptide stability, potentially informing the design of more robust therapeutic candidates and improving the predictability of in vivo performance.
Bioanalytical Method Development: Linaclotide D4 serves as an indispensable internal standard in the development and validation of bioanalytical assays. Its isotopic distinction enables the accurate calibration of mass spectrometry-based quantification methods, ensuring the reliable measurement of linaclotide and its metabolites in biological fluids. This application is fundamental for supporting preclinical and translational research, where precise analytical data are essential for interpreting experimental outcomes.
Drug-Drug Interaction Studies: The use of Linaclotide D4 in drug-drug interaction research allows for the detailed investigation of potential metabolic or transporter-mediated interactions with co-administered compounds. By incorporating this labeled analog into experimental protocols, researchers can distinguish between the pharmacokinetic behavior of linaclotide and other substances, thereby clarifying mechanisms of interaction and informing the development of safer combination therapies.
Receptor Binding and Mechanistic Investigations: Linaclotide D4 is also instrumental in receptor binding studies and mechanistic explorations involving the GC-C signaling pathway. Its traceable properties facilitate the precise mapping of binding sites and the quantification of receptor-ligand interactions in cellular models. Such research deepens the understanding of GC-C agonist activity and supports the rational design of novel modulators targeting gastrointestinal physiology.
Peptide Therapeutic Research: In the broader context of peptide drug discovery, Linaclotide D4 functions as a model system for evaluating the impact of isotopic labeling on biological activity and pharmacological properties. Researchers leverage its unique features to explore structure-activity relationships, investigate degradation pathways, and refine synthetic methodologies. Through these multifaceted applications, Linaclotide D4 continues to advance the frontiers of carbohydrate-peptide research, offering valuable insights that drive innovation in therapeutic development.
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