| Name | Linaclotide |
| Description | Linaclotide, developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, is a potent and selective guanylate cyclase C agonist. |
| In vitro | Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine, inhibit sodium ion absorption, enhance water secretion into the lumen, and improve defecation; the drug is minimally absorbed into the systemic circulation[2]. In vitro, linaclotide inhibits [125I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner, while binding to membranes from GC-C null mice significantly decreases. Linaclotide is completely degraded after a 30-minute incubation in jejunal fluid in vitro[1]. |
| In vivo | Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation [2]. Pharmacokinetic analysis shows very low oral bioavailability (0.10%). In intestinal secretion and transit models, linaclotide exhibits significant pharmacological effects in wt, but not in GC-C null mice: increased fluid secretion into surgically ligated jejunal loops is accompanied by elevated cyclic guanosine-3',5-monophosphate levels and accelerated gastrointestinal transit [1]. |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 20 mg/mL (13.1 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (1.31 mM), Sonication is recommended.
DMSO : 150 mg/mL (98.25 mM)
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| Keywords | Linaclotide | Inhibitor | inhibit | Guanylatecyclase | Guanylate Cyclase |
| Inhibitors Related | LY83583 | Lificiguat | Sinitrodil | NPR-C activator 1 | Riociguat | Nelociguat | Nitroprusside disodium dihydrate | Vericiguat | NS-2028 | Methylene Blue | Methylene Blue trihydrate | Cinaciguat |
| Related Compound Libraries | Cyclic Peptide Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Peptide Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
