Linaclotide

Modify Date: 2024-01-02 14:56:00

Linaclotide Structure
Linaclotide structure
 Common Name Linaclotide
CAS Number 851199-59-2 Molecular Weight 1526.736
Density 1.6±0.1 g/cm3 Boiling Point 2045.0±65.0 °C at 760 mmHg
Molecular Formula C59H79N15O21S6 Melting Point N/A
MSDS N/A Flash Point 1190.5±34.3 °C

 Use of Linaclotide


Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.

 Names

Name linaclotide
Synonym More Synonyms

 Linaclotide Biological Activity

Description Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
Related Catalog
In Vitro 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]. 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].
In Vivo 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]. Linaclotide significantly increases weekly spontaneous bowel movements and complete spontaneous bowel movements (CSBMs) while reducing abdominal pain in patients with chronic constipation[2].
Animal Admin 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].
References

[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.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 2045.0±65.0 °C at 760 mmHg
Molecular Formula C59H79N15O21S6
Molecular Weight 1526.736
Flash Point 1190.5±34.3 °C
Exact Mass 1525.389893
PSA 725.71000
LogP -5.84
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.712

 Synonyms

Linzess
Linaelotide Acetate
L-Tyrosine, 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-, cyclic (1→6),(2→10),(5→13)-tris(disulfide)
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)
Constella
Linaclotide
LINACLOTIDE ACETATE
Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (disulfide bridge: 1-6; 2-10; 5-13)
N-({(1R,4S,7S,13S,16R,21R,24R,27S,30S,33R,38R,44S)-21-Amino-13-(2-amino-2-oxoethyl)-27-(2-carboxyethyl)-30-(4-hydroxybenzyl)-44-[(1R)-1-hydroxyethyl]-4-methyl-3,6,12,15,22,25,28,31,40,43,46,51-dodecao ;xo-18,19,35,36,48,49-hexathia-2,5,11,14,23,26,29,32,39,42,45,52-dodecaazatetracyclo[22.22.4.2.0]dopentacont-38-yl}carbonyl)-L-tyrosine
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Related Compounds: More...
Linaclotide acetate
851199-60-5
Chemsrc provides Linaclotide(CAS#:851199-59-2) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of Linaclotide are included as well.>> amp version: Linaclotide

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