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Linaclotide

Catalog No. T11852 CAS 851199-59-2

Linaclotide developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, and is a potent and selective <a href="/target/Guanylate_cyclase" style="display: inline; color: #c13a36">Guanylate cyclase</a> C agonist.

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Linaclotide, CAS 851199-59-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 92.00
5 mg	In stock	$ 140.00
10 mg	In stock	$ 233.00
25 mg	In stock	$ 412.00
50 mg	In stock	$ 619.00
100 mg	In stock	$ 942.00

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Purity: 97.93%

Purity: 98.71%

Biological Description

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Storage & Solubility Information

Description	Linaclotide developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation, and is a potent and selective guanylate cyclase C agonist.
In vitro	Linaclotide acts on guanylate cyclase-C receptors on the luminal membrane to increase chloride and bicarbonate secretions into the intestine and inhibit the absorption of sodium ions, thus increasing the secretion of water into the lumen and improving defecation;?the drug is minimally absorbed into the systemic circulation[2].Linaclotide inhibits in vitro [125I]-STa binding to intestinal mucosal membranes from wt mice in a concentration-dependent manner.?In contrast, [125I]-STa binding to these membranes from GC-C null mice is significantly decreased.?After incubation in vitro in jejunal fluid for 30 min, linaclotide is completely degraded[1].
In vivo	Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation[2].Pharmacokinetic analysis shows very low oral bioavailability (0.10%).?In intestinal secretion and transit models, linaclotide exhibits significant pharmacological effects in wt, but not in GC-C null mice: induction of increased fluid secretion into surgically ligated jejunal loops is accompanied by the secretion of elevated levels of cyclic guanosine-3',5-monophosphate and accelerated gastrointestinal transit[1].

Molecular Weight	1526.74
Formula	C59H79N15O21S6
CAS No.	851199-59-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 20 mg/mL (13.10 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

NO PAINS Compound Library Anti-Cancer Drug Library Macrocyclic Compound Library Peptide Compound Library Preclinical Compound Library ReFRAME Related Library Orally Active Compound Library Anti-Cancer Approved Drug Library Cyclic Peptide Library Anti-Cancer Clinical Compound Library

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Keywords

Linaclotide 851199-59-2 GPCR/G Protein Guanylate cyclase Inhibitor Guanylate Cyclase inhibit inhibitor

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