1. GPCR/G Protein
  2. Guanylate Cyclase

Linaclotide 

Cat. No.: HY-17584 Purity: 98.96%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
Linaclotide Chemical Structure

Linaclotide Chemical Structure

CAS No. : 851199-59-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO $420 In-stock
5 mg $150 In-stock
10 mg $250 In-stock
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02220348 Forest Laboratories Breast Feeding|Constipation|Irritable Bowel Syndrome July 2014 Phase 1
NCT02465385 University of Virginia Crohn's|Ulcerative Colitis|Gastrointestinal Bleeding February 2015 Phase 4
NCT01950403 Mayo Clinic|National Cancer Institute (NCI) Colorectal Cancer|Healthy, no Evidence of Disease September 2013 Phase 1
NCT02078323 Augusta University|Forest Laboratories Irritable Bowel Syndrome With Constipation (IBS-C) February 2014
NCT02270983 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Opioid-Induced Constipation October 2014 Phase 2
NCT02590432 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Irritable Bowel Syndrome With Constipation|Chronic Idiopathic Constipation November 2015 Phase 4
NCT03119584 Texas Tech University Health Sciences Center, El Paso Chronic Constipation in Diabetic Patients September 1, 2015 Phase 4
NCT02291679 Ironwood Pharmaceuticals, Inc.|Forest Laboratories Chronic Idiopathic Constipation October 2014 Phase 3
NCT00948818 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Irritable Bowel Syndrome Characterized by Constipation July 2009 Phase 3
NCT01642914 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Chronic Constipation|Constipation August 2012 Phase 3
NCT00938717 Ironwood Pharmaceuticals, Inc.|Forest Laboratories Irritable Bowel Syndrome With Constipation July 2009 Phase 3
NCT00765999 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Chronic Constipation|Irritable Bowel Syndrome With Constipation October 2008 Phase 3
NCT00730171 Ironwood Pharmaceuticals, Inc.|Forest Laboratories Irritable Bowel Syndrome With Constipation|Chronic Constipation September 2008 Phase 3
NCT02837783 Ironwood Pharmaceuticals, Inc.|University Hospital of South Manchester NHS Foundation Trust Irritable Bowel Syndrome Characterized by Constipation July 2016 Phase 4
NCT00765882 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Chronic Constipation September 2008 Phase 3
NCT02559570 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Functional Constipation in Children Ages 6-17 Years November 30, 2015 Phase 2
NCT02559817 Forest Laboratories|Ironwood Pharmaceuticals, Inc. Irritable Bowel Syndrome With Constipation November 1, 2015 Phase 2
NCT00730015 Ironwood Pharmaceuticals, Inc.|Forest Laboratories Chronic Constipation August 2008 Phase 3
NCT00402337 Ironwood Pharmaceuticals, Inc. Chronic Constipation November 2006 Phase 2
NCT00460811 Ironwood Pharmaceuticals, Inc. Irritable Bowel Syndrome With Constipation April 2007 Phase 2
NCT01880424 AstraZeneca|Ironwood Pharmaceuticals, Inc. Irritable Bowel Syndrome With Constipation (IBS-C) July 2013 Phase 3
NCT02559206 Ironwood Pharmaceuticals, Inc.|Forest Laboratories Irritable Bowel Syndrome With Constipation October 2015 Phase 2
NCT02360384 Wingate Institute of Neurogastroenterology Irritable Bowel Syndrome November 2015
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 0.6550 mL 3.2750 mL 6.5499 mL
5 mM 0.1310 mL 0.6550 mL 1.3100 mL
10 mM 0.0655 mL 0.3275 mL 0.6550 mL
Animal Administration
[1]

Mouse: 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1526.74

Formula

C₅₉H₇₉N₁₅O₂₁S₆

CAS No.

851199-59-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Linaclotide
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