Description

Linaclotide acetate (CAS 851199-60-5) is a synthetic, tetradecapeptide and potent, highly selective agonist of guanylate cyclase-C (GC-C) receptors in the intestinal epithelium. Functioning locally in the gut, Linaclotide activates GC-C to elevate intracellular and extracellular cyclic GMP (cGMP), promoting secretion of chloride, bicarbonate, and water into the lumen, thereby accelerating gastrointestinal transit and improving bowel movement frequency and consistency.
Additionally, elevated extracellular cGMP inhibits colonic nociceptors, providing relief from abdominal pain and visceral hypersensitivity . Clinical and preclinical studies demonstrate Linaclotide acetate’s efficacy in alleviating symptoms of IBS-C and chronic constipation, with favorable safety and minimal systemic bioavailability.

Product Specifications

Mechanism of Action & Research Applications

Mechanism of Action

Linaclotide acetate activates the GC-C receptor present on intestinal epithelial cells, increasing levels of cGMP. This stimulates chloride and bicarbonate secretion through CFTR, inhibits sodium absorption, and increases water secretion into the gut—thus enhancing motility and relieving constipation. Additionally, extracellular cGMP reduces visceral pain by modulating colonic sensory afferents .

Research Applications

• IBS-C & Chronic Constipation Models – Assess improvements in stool formation, frequency, and transit.

• GI Secretion Studies – Model electrolyte and fluid transport dynamics via GC-C activation.

• Visceral Pain Assays – Evaluate analgesic effects through modulation of nociceptors.

• Gut Physiology Research – Explore novel GC-C-mediated pathways for motility and neurogastroenterology.

Development & Formulation Notes

Stock Solutions & Handling

Reconstitute with sterile water or buffer; sonication or gentle heating may enhance solubility. Prepare fresh for each experiment. Use low-binding labware and filter (0.22 µm) if sterility is required.

Assay Design

Design dose–response assays to measure cGMP, chloride secretion, or pain-related behaviors. Include time-course studies and proper controls.

Combination & Pathway Mapping

Combine with other gut-targeted compounds (e.g., CFTR modulators) to dissect overlapping mechanisms or synergy in secretion, motility, or pain relief.

Disclaimer

Linaclotide acetate is strictly for laboratory research use only. It is not a medical, pharmaceutical, or veterinary product and is not approved for human consumption. Handle under appropriate laboratory biosafety standards and dispose of per local guidelines. The information herein reflects preclinical and clinical research contexts; users must verify suitability for their experimental applications.

Keywords

Linaclotide acetate; GC-C agonist peptide; guanylate cyclase-C activator; IBS-C research; chronic constipation research; cGMP stimulating peptide; visceral analgesia peptide; GMP peptide; CAS 851199-60-5; research-use-only.

Packaging & Availability

• Standard Packs: 1 mg, 5 mg, 10 mg (custom sizes available)

• Bulk/Wholesale: Multi-gram lots available with batch reservation and scheduled supply options

• Documentation: Each lot includes CoA, HPLC trace, and MS identity; extended QC available for audits

Quality Assurance

Produced under GMP-compliant processes. Batch testing ensures identity (MS), purity (HPLC), moisture content, and appearance. Stability recommendations and solubility data accompany each lot; endotoxin testing available upon request.

Custom Services

• Custom labeling and aliquoting to suit LIMS or ELN integration

• Formulation guidance for aqueous or buffer systems

• Stability study consulting for storage/shipment conditions

• Protocol design to support motility or analgesia research models