Linaclotide

DESCRIPTION

A peptide agonist of the guanylate cyclase C receptor (Ki = 16.4 nM in a radioligand binding assay using mouse intestinal mucosa); stimulates fluid secretion and cGMP concentration in jejunal loops isolated from wild-type mice but not guanylate cyclase C receptor-null mice; increases intestinal transit rate in wild-type mice when administered at a dose of 100 μg/kg; 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

DETAILS

Inchi: InChI=1S/C59H79N15O21S6/c1-26-47(82)69-41-25-101-99-22-38-52(87)65-33(13-14-45(80)81)49(84)66-34(16-28-5-9-30(76)10-6-28)50(85)71-40(54(89)72-39(23-97-96-20-32(60)48(83)70-38)53(88)67-35(18-43(61)78)58(93)74-15-3-4-42(74)56(91)63-26)24-100-98-21-37(64-44(79)19-62-57(92)46(27(2)75)73-55(41)90)51(86)68-36(59(94)95)17-29-7-11-31(77)12-8-29/h5-12,26-27,32-42,46,75-77H,3-4,13-25,60H2,1-2H3,(H2,61,78)(H,62,92)(H,63,91)(H,64,79)(H,65,87)(H,66,84)(H,67,88)(H,68,86)(H,69,82)(H,70,83)(H,71,85)(H,72,89)(H,
Purity: ≥95%
Raptas: Product Type|Biochemicals|Peptides||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Gastric Disease|Crohn's Disease||Research Area|Immunology & Inflammation|Gastric Disease|Ulcerative Colitis||Research Area|Neuroscience|Pain Research
Smiles: N[C@H](C(N[C@]1([H])C(N[C@H](CCC(O)=O)C2=O)=O)=O)CSSC[C@]([H])(NC3=O)C(N[C@@H](CC(N)=O)C(N4[C@@](C(N[C@H](C(N[C@](CSSC1)([H])C(NC([C@H](O)C)C(NCC(N[C@H](C(N[C@@H](CC5=CC=C(O)C=C5)C(O)=O)=O)CSSC[C@]3([H])NC([C@H](CC6=CC=C(O)C=C6)N2)=O)=O)=O)=O)=O)C)=O)([H])CCC4)=O)=O
Inchikey: KXGCNMMJRFDFNR-VRMHCMCOSA-N
Cas Number: 851199-59-2
Formulation: A solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C59H79N15O21S6
Formula Weight: 1526.7
Shelf Life Days: 1460