1. GPCR/G Protein
  2. Guanylate Cyclase
  3. Linaclotide


Cat. No.: HY-17584 Purity: 98.44%
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 Water USD 504 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 300 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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
Molecular Weight







O=C([[email protected]@H](NC([[email protected]@](CSSC[[email protected]@H]1N)([H])NC([[email protected]@](CSSC[[email protected]](N2)C(N[[email protected]](C(O)=O)CC3=CC=C(O)C=C3)=O)([H])NC([[email protected]@H](NC([[email protected]@H](N4)CCC(O)=O)=O)CC5=CC=C(O)C=C5)=O)=O)=O)CC(N)=O)N6[[email protected]@](C(N[[email protected]](C(N[[email protected]](CSSC[[email protected]](C4=O)([H])NC1=O)([H])C(NC(C(NCC2=O)=O)[[email protected]](O)C)=O)=O)C)=O)([H])CCC6


Room temperature in continental US; may vary elsewhere.

Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
Animal Administration

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].

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


Purity: 98.44%

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