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Linaclotide-d4
Linaclotide-d4
Artikelnummer
CAY28798
Verpackungseinheit
500 µg
Hersteller
Cayman Chemical
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Formulation: A solid
Formal Name: ((3S,6R,15R,20R,23S,26R,29R,32R,37R,40S,45aS)-32-amino-40-(2-amino-2-oxoethyl)-26-(2-carboxyethyl)-23-(4-hydroxybenzyl)-9-((R)-1-hydroxyethyl)-3-(methyl-d3)-1,4,7,10,13,22,25,28,31,38,41,47-dodecaoxotetracontahydro-19H-37,20-(epiminomethano)-6,29-(methanodithiomethano)pyrrolo[2,1-s][1,2,27,28]tetrathia[5,8,11,14,17,20,23,32,35,38,41]undecaazacyclotritetracontine-15-carbonyl-3-d)-L-tyrosine
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C59H75D4N15O21S6
Formula Weight: 1530,8
Shelf life (days): 1460
Notes: Linaclotide-d4 is intended for use as an internal standard for the quantification of linaclotide (Item No. 24085) by GC- or LC-MS. 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.
Formal Name: ((3S,6R,15R,20R,23S,26R,29R,32R,37R,40S,45aS)-32-amino-40-(2-amino-2-oxoethyl)-26-(2-carboxyethyl)-23-(4-hydroxybenzyl)-9-((R)-1-hydroxyethyl)-3-(methyl-d3)-1,4,7,10,13,22,25,28,31,38,41,47-dodecaoxotetracontahydro-19H-37,20-(epiminomethano)-6,29-(methanodithiomethano)pyrrolo[2,1-s][1,2,27,28]tetrathia[5,8,11,14,17,20,23,32,35,38,41]undecaazacyclotritetracontine-15-carbonyl-3-d)-L-tyrosine
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C59H75D4N15O21S6
Formula Weight: 1530,8
Shelf life (days): 1460
Notes: Linaclotide-d4 is intended for use as an internal standard for the quantification of linaclotide (Item No. 24085) by GC- or LC-MS. 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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Gernot Ensinger, M.Sc.
Laurent Haze
