Linaclotide acetate is an oral guanylate cyclase C agonist linaclotide. It is 14 amino acid peptide for the potential treatment of constipation-predominant irritable bowel syndrome and chronic idiopathic constipation.
CAT No: R1947
CAS No:851199-60-5
Synonyms/Alias:Linaclotide acetate;851199-60-5;MD-1100 acetate;MM-416775;UNII-NSF067KU1M;Linaclotide acetate [USAN];Linaclotide acetate (USAN);MD-1100;NSF067KU1M;MM 416775;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), monoacetate (salt);CHEMBL3301676;DTXSID60583223;PUBCHEM_16158207;AKOS040733602;AT42588;FL65062;D06612;
Chemical Name:acetic acid;(2S)-2-[[(1R,4S,7S,13S,16R,21R,24R,27S,30S,33R,38R,44S)-21-amino-13-(2-amino-2-oxoethyl)-27-(2-carboxyethyl)-44-[(1R)-1-hydroxyethyl]-30-[(4-hydroxyphenyl)methyl]-4-methyl-3,6,12,15,22,25,28,31,40,43,46,51-dodecaoxo-18,19,35,36,48,49-hexathia-2,5,11,14,23,26,29,32,39,42,45,52-dodecazatetracyclo[22.22.4.216,33.07,11]dopentacontane-38-carbonyl]amino]-3-(4-hydroxyphenyl)propanoic acid
Linaclotide acetate is a synthetic peptide and guanylate cyclase-C (GC-C) agonist that has garnered significant attention in biochemical research due to its unique structure and mechanism of action. As a 14-amino acid peptide, it is structurally related to endogenous guanylin and uroguanylin, and is stabilized as an acetate salt for enhanced handling and solubility in laboratory settings. The compound's ability to modulate intracellular cyclic guanosine monophosphate (cGMP) levels through GC-C receptor activation has made it a valuable tool for elucidating pathways involved in fluid and electrolyte homeostasis within the gastrointestinal tract. Its robust activity, stability, and well-characterized pharmacology have positioned it as a model system for studies in peptide signaling, intestinal physiology, and receptor-ligand interactions.
Peptide signaling research: Linaclotide acetate serves as a powerful probe for dissecting the molecular mechanisms of GC-C receptor activation and downstream signaling events. Researchers utilize it to study the dynamics of cGMP production and the subsequent modulation of ion transporters such as the cystic fibrosis transmembrane conductance regulator (CFTR). By applying this synthetic peptide to in vitro cell systems or ex vivo tissue models, investigators can map the influence of GC-C agonism on epithelial ion flux, barrier function, and fluid secretion, facilitating a deeper understanding of intestinal homeostasis and related pathophysiological processes.
Structure-activity relationship (SAR) studies: The defined sequence and disulfide-rich architecture of linaclotide acetate make it an ideal template for SAR investigations in peptide engineering. Scientists employ it as a reference compound to explore the impact of amino acid substitutions, backbone modifications, and alternative cyclization strategies on GC-C receptor affinity and selectivity. Such studies not only elucidate the determinants of peptide-receptor interaction but also inform the rational design of novel analogs with tailored pharmacological profiles for research applications.
Intestinal transport and permeability assays: In experimental models of epithelial transport, linaclotide acetate is frequently used to induce and quantify changes in transepithelial ion movement and water flux. Its well-characterized action on GC-C enables the controlled modulation of chloride and bicarbonate secretion, providing a reproducible system for evaluating intestinal barrier integrity, nutrient absorption, and the effects of pharmacological inhibitors or enhancers. These assays are instrumental in advancing knowledge of gut physiology and the interplay between peptide hormones and epithelial function.
Analytical method development: The distinct physicochemical properties of linaclotide acetate, including its peptide nature and stability as an acetate salt, make it a valuable standard for developing and validating analytical techniques such as high-performance liquid chromatography (HPLC) and mass spectrometry. Laboratories leverage its defined mass and retention characteristics to optimize detection protocols for peptide-based analytes, assess method sensitivity, and ensure reproducibility in quantifying synthetic or endogenous GC-C agonists across diverse sample matrices.
Peptide formulation and delivery research: As a representative synthetic peptide with established bioactivity, linaclotide acetate is utilized in studies focused on peptide stabilization, formulation strategies, and delivery system development. Its use in evaluating the impact of excipients, encapsulation technologies, and release kinetics provides critical insights into the challenges and solutions associated with peptide drug delivery for research purposes. These investigations support the advancement of peptide-based therapeutics and the broader field of biopharmaceutical formulation science.
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