| Bioactivity | Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation. | ||||||
| Invitro | Linaclotide inhibits in vitro [125I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner. In contrast, [125I]-STa binding to these membranes from GC-C null mice is significantly decreased. After incubation in vitro in jejunal fluid for 30 min, linaclotide is completely degraded[1]. Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine and inhibit the absorption of sodium ions, thus increasing the secretion of water into the lumen and improving defecation; the drug is minimally absorbed into the systemic circulation[2]. | ||||||
| Name | Linaclotide | ||||||
| CAS | 851199-59-2 | ||||||
| Formula | C59H79N15O21S6 | ||||||
| Molar Mass | 1526.74 | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Linaclotide
CAS: 851199-59-2 F: C59H79N15O21S6 W: 1526.74
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predomina
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