Linaclotide

A peptide agonist of the guanylate cyclase C receptor

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2mg

￥1087.00

870.00

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5mg

￥1612.00

1290.00

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10mg

￥2700.00

2160.00

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货号: ajce44274
CAS: 851199-59-2
别名: 利那洛肽
分子式: C59H79N15O21S6
分子量: 1526.74
纯度: >98%
溶解度: Water : 20 mg/mL (13.10 mM) ; DMSO : 50 mg/mL(32.75 mM)
储存: Store at -20° C
库存: 现货

Background

Linaclotide is a peptide agonist of the guanylate cyclase C receptor (K_i = 16.4 nM in a radioligand binding assay using mouse intestinal mucosa).¹ 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.² Formulations containing linaclotide have been used for the treatment of constipation and pain associated with irritable bowel syndrome.

1.Bryant, A.P., Busby, R.W., Bartolini, W.P., et al.Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tractLife Sci.86(19-20)760-765(2010) 2.Castro, J., Harrington, A.M., Hughes, P.A., et al.Linaclotide inhibits colonic nociceptors and relieves abdominal pain via guanylate cyclase-C and extracellular cyclic guanosine 3',5'-monophosphateGastroenterology145(6)1334-1346(2013)

Protocol

Animal experiment:

Mice: To determine oral bioavailability, three groups (n=3) of female CD-1 mice receive linaclotide (8 mg/kg) intravenously (i.v.), while two groups (n=3) receive linaclotide (8 mg/kg) by gavage (p.o.). Blood is allowed to clot for 5 min, centrifuged at 13,000×g for 3 min, and the serum is collected and stored at ?80 °C until sample preparation and analysis by LC-MS/MS[1].

参考文献:

[1]. Bryant AP, et al. Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract. Life Sci. 2010 May 8;86(19-20):760-5.
[2]. Love BL, et al. Linaclotide: a novel agent for chronic constipation and irritable bowel syndrome. Am J Health Syst Pharm. 2014 Jul 1;71(13):1081-91.