Linaclotide
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[ Sequence ] H-Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr-OH cyclic(1-6),(2-10),(5-13)-tris(disulfide)
[ Cas NO. ] 851199-59-2
[ Molecular Formula ] C59H79N15O21S6
[ Molecular Weight ] 1526.73
[ Appearance ] White Powder
[ Purity ] 98%
[ Application ]
For the study of irritable bowel syndrome with constipation (IBS-C) and chronic constipation.
About Linaclotide
Linaclotide is a guanylate cyclase-C receptor agonist (GCCA) with both visceral analgesic and endocrine activity. Both linaclotide and its active metabolites can bind to guanylate cyclase-C (GC-C) receptors on the luminal surface of the small intestinal epithelium. In animal models, through the activation of GC-C, linaclotide can reduce visceral pain and improve gastrointestinal transit speed. In humans, the drug can also increase intestinal transit speed. The result of GC-C activation is increased intracellular and extracellular cGMP (cyclic guanosine monophosphate) concentrations. Extracellular cGMP can reduce the activity of pain nerve fibers and relieve visceral pain in model animals. Intracellular cGMP can increase the secretion of chloride and bicarbonate in the lumen of the small intestine by activating CFTR (cystic fibrosis transmembrane conductance regulator), which eventually leads to increased secretion of small intestinal fluid and faster intestinal transit.
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