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: 10-101-161
CAS No:851199-59-2
Synonyms/Alias:Linaclotide;Linzess;851199-59-2;Constella;UNII-N0TXR0XR5X;Linaclotida;HSDB 8224;Linaclotide [USAN:INN];N0TXR0XR5X;ASP 0456;CHEBI:68551;ASP0456;ASP-0456;DTXSID90234256;L-Tyrosine, L-cysteinyl-L-cysteinyl-L-alpha-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-, cyclic (1->6),(2->10),(5->13)-tris(disulfide);Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (disulfide bridge: 1-6; 2-10; 5-13);L-cysteinyl-L-cysteinyl-L-alpha-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-L-tyrosine cyclic (1->6),(2->10),(5->13)-tris(disulfide);linaclotidum;Constella (TN);L-Tyrosine, L-cysteinyl-L-cysteinyl-L-a-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-, cyclic (1?6),(2?10),(5?13)-tris(disulfide); Linaclotide; Linzess;Linzess (TN);Linzess Ammonium Salt;Linaclotide (JAN/USAN);GTPL5017;CHEMBL3301675;SCHEMBL13114620;A06AX04;DTXCID90156747;GLXC-13151;EX-A6257;DB08890;NCGC00389841-01;DA-54931;FL138962;D09355;Q3832559;(9-L-TYROSINE)HEAT-STABLE ENTEROTOXIN (ESCHERICHIA COLI)-(6-19)-PEPTIDE;L-Tyrosine, L-cysteinyl-L-cysteinyl-L-alpha-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-, cyclic (1->6), (2->10), (5->13)-tris(disulfide);
Linaclotide is a synthetic peptide compound that functions as a potent agonist of the guanylate cyclase-C (GC-C) receptor, structurally modeled after endogenous guanylin and uroguanylin peptides. Distinguished by its 14-amino acid sequence and three disulfide bridges, linaclotide exhibits high stability and bioactivity in gastrointestinal environments. Its unique molecular architecture and mechanism of action have established it as a valuable tool in the study of cyclic guanosine monophosphate (cGMP)-mediated signaling pathways and epithelial transport processes. As a research-grade peptide, linaclotide serves as a reference compound for elucidating the roles of GC-C activation in fluid homeostasis, ion transport, and barrier function across epithelial tissues.
Peptide signaling research: Linaclotide is widely utilized in studies investigating the molecular mechanisms of peptide-mediated signaling within the gastrointestinal tract. By selectively activating the GC-C receptor, it enables researchers to dissect downstream pathways involving cGMP production, protein kinase activation, and ion channel modulation. These investigations are critical for understanding how peptide hormones regulate intestinal secretion, absorption, and cellular communication, offering insights into the physiological balance of fluid and electrolytes.
Epithelial transport and barrier function studies: The compound is instrumental in experimental models examining the regulation of epithelial ion transport and barrier integrity. Through its ability to stimulate cGMP synthesis and modulate chloride and bicarbonate secretion via the cystic fibrosis transmembrane conductance regulator (CFTR), linaclotide provides a robust platform for characterizing epithelial responses to peptide agonists. Such research supports the development of in vitro and ex vivo systems for studying mucosal defense mechanisms and the molecular basis of epithelial permeability.
Drug discovery and pharmacological profiling: Linaclotide serves as a reference peptide in high-throughput screening assays and pharmacological profiling aimed at identifying novel GC-C agonists or modulators. Its well-characterized activity profile allows for benchmarking the efficacy and selectivity of new compounds targeting the same receptor pathway. This application is particularly valuable in the early stages of drug discovery, where comparative analyses inform lead optimization and structure-activity relationship studies.
Peptide synthesis and analytical method development: The unique disulfide-rich structure of linaclotide makes it an exemplary model for peptide synthesis, folding, and analytical characterization. Researchers employ it to refine solid-phase peptide synthesis protocols, optimize oxidative folding conditions, and validate analytical techniques such as HPLC, mass spectrometry, and NMR spectroscopy. These methodological advancements contribute to the broader field of peptide chemistry, facilitating the production and quality assessment of complex peptide molecules.
Gastrointestinal physiology research: As a stable and selective GC-C agonist, linaclotide is frequently used to probe the physiological roles of guanylin peptides in gut function. Its application extends to studies investigating the regulation of intestinal motility, secretion, and sensory signaling in normal and pathophysiological states. By enabling precise modulation of GC-C activity, linaclotide advances the understanding of gastrointestinal homeostasis and the interplay between epithelial cells and the enteric nervous system.
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