Formulation: A solid
Formal Name: L-cysteinyl-L-cysteinyl-L-α-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)
Purity: ≥95%
Formula Markup: C59H79N15O21S6
Formula Weight: 1526,7
Shelf life (days): 1460
CAS Number: 851199-59-2
Notes: Linaclotide is a peptide agonist of the guanylate cyclase C receptor (Ki = 16.4 nM in a radioligand binding assay using mouse intestinal mucosa).{40472} Luminal exposure to 5 μg of linaclotide stimulates fluid secretion and cGMP concentration in jejunal loops isolated from wild-type mice but not guanylate cyclase C receptor-null mice. Linaclotide (100 μg/kg) increases intestinal transit rate in wild-type mice. It also reduces the number of phosphorylated ERK-positive dorsal horn neurons in the thoracolumbar spinal cord, a marker of nociceptive signaling, following noxious colorectal distension and mechanical hypersensitivity in a mouse model of TNBS-induced colitis.{40473} Formulations containing linaclotide have been used for the treatment of constipation and pain associated with irritable bowel syndrome.
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