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 that functions as an agonist of the guanylate cyclase-C (GC-C) receptor, structurally modeled after endogenous guanylin peptides. This compound is characterized by its 14-amino acid sequence and distinctive three disulfide bonds, conferring high stability and selectivity for the GC-C receptor found on the luminal surface of the intestinal epithelium. Linaclotide's unique mode of action involves the activation of intracellular cyclic guanosine monophosphate (cGMP) pathways, which modulate ion and fluid transport in the gastrointestinal tract. Its molecular design enables robust resistance to proteolytic degradation, making it an attractive molecule for research in gastrointestinal physiology, pharmacology, and peptide engineering. The compound's ability to influence fluid homeostasis, visceral pain signaling, and epithelial barrier function has positioned it as a valuable tool in both basic and applied scientific investigations.
Gastrointestinal Motility Research: Linaclotide plays a pivotal role in the study of gastrointestinal motility disorders, particularly through its capacity to stimulate chloride and bicarbonate secretion via CFTR (cystic fibrosis transmembrane conductance regulator) activation. By elevating cGMP levels, it enhances intestinal fluid secretion, thereby facilitating stool passage and providing a model for investigating mechanisms underlying constipation and dysmotility syndromes. Researchers utilize this peptide to dissect the cellular and molecular pathways that govern electrolyte transport, epithelial hydration, and peristaltic reflexes, generating insights into gut function and dysfunction.
Visceral Pain Mechanisms: The peptide is extensively employed in research focused on visceral pain and hypersensitivity, which are hallmarks of various functional gastrointestinal disorders. By modulating extracellular cGMP levels, linaclotide has been shown to reduce the excitability of nociceptive sensory neurons within the gut wall. This property allows scientists to explore the neurochemical and electrophysiological bases of pain signaling in the enteric nervous system, as well as to evaluate novel therapeutic approaches for alleviating abdominal discomfort and hyperalgesia.
Epithelial Barrier Function: Investigations into intestinal barrier integrity frequently incorporate linaclotide due to its influence on epithelial tight junctions and permeability. By activating GC-C and downstream signaling cascades, the peptide contributes to the maintenance of mucosal barrier function, which is critical for protecting against luminal pathogens and toxins. Researchers leverage its modulatory effects to assess barrier dysfunction in models of inflammatory and functional bowel diseases, facilitating the identification of targets for restoring epithelial resilience.
Peptide Drug Development: Linaclotide serves as a template for the design and optimization of next-generation peptide therapeutics targeting GC-C and related receptors. Its structural features, including disulfide bond patterns and receptor selectivity, provide a framework for engineering analogs with enhanced bioactivity, stability, or tissue specificity. The compound is utilized in structure-activity relationship studies, peptide synthesis optimization, and high-throughput screening platforms aimed at discovering novel agents for gastrointestinal and other systemic indications.
Signal Transduction Studies: The ability of linaclotide to precisely activate cGMP-dependent signaling pathways makes it indispensable in research examining intracellular messenger systems. Scientists apply this peptide to delineate the downstream effects of GC-C activation, including the regulation of ion channels, transporter proteins, and gene expression profiles. Such studies contribute to a broader understanding of how cyclic nucleotide signaling orchestrates cellular physiology in both normal and pathological contexts.
In summary, linaclotide stands out as a versatile research tool with wide-ranging applications in gastrointestinal motility, pain signaling, epithelial barrier function, peptide drug development, and signal transduction studies. Its unique structural and functional properties continue to drive innovation in the exploration of gut physiology and the development of targeted therapeutic strategies.
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