85-2027-33　Linaclotide 1mg　CAS No:851199-59-2　164757

特徴

• 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-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)
• 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 -20°C. Reconstituted product is stable for 24 hours. Store at -20°C. 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.