Linaclotide is a peptide agonist of the guanylate cyclase C receptor (Ki = 16.4nM in a radioligand binding assay using mouse intestinal mucosa).1 Luminal exposure to 5ug 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 (100ug/kg) increases intestinal transit 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.2 Formulations containing linaclotide have been used for the treatment of constipation and pain associated with irritable bowel syndrome. Synonyms: 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-L-tyrosine Cyclic (16),(210),(513)-Tris(disulfide) CAS Number: 851199-59-2 Molecular Formula: C59H79N15O21S6 Molecular Weight: 1526.74 Purity: 95% Appearance: White solid Melting Point: >249 (dec) (lit) Solubility: DMSO (Slightly), Water (Very Slightly) Storage and Stability: Lyophilized product is stable for 6 months after receipt at -20C. Reconstituted product is stable for 24 hours. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer. Hygroscopic. Store under inert atmosphere.
Molecular Weight:
1526.74
CAS Number:
[851199-59-2]
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