Linaclotide Research Peptide (RUO)

What is Linaclotide?

Linaclotide is a minimally absorbed, locally acting 14-amino-acid synthetic peptide agonist of guanylate cyclase-C (GC-C). Its sequence (Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr) is constrained by three intramolecular disulfide bridges, a folding pattern that is essential to its activity and the central synthesis challenge of the molecule. It acts locally on the luminal surface of the intestinal epithelium: binding to transmembrane GC-C receptors elevates intracellular and extracellular cyclic GMP (cGMP), which stimulates chloride and bicarbonate secretion (largely via CFTR), increasing intestinal fluid and accelerating transit.

As an active pharmaceutical ingredient, linaclotide (CAS 851199-59-2, molecular formula C59H79N15O21S6, ~1526.74 g/mol) is typically presented as a lyophilised powder. It is approved by the US FDA and the EMA for irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation.

How Linaclotide Is Produced & Characterised

Linaclotide is a synthetically demanding peptide: six cysteine residues must form three specific disulfide bonds (1-6, 2-10, 5-13), and incorrect pairing produces inactive disulfide isomers that are difficult to separate. In industry, the molecule is generally prepared by Fmoc solid-phase peptide synthesis (SPPS), followed by a controlled oxidative folding step that drives formation of the correct three-disulfide topology, then purification on preparative dynamic axial compression (DAC) HPLC columns to resolve the target from misfolded and deletion-sequence impurities.

Characterisation typically combines UPLC/HPLC for purity, LC-MS for sequence and disulfide-connectivity confirmation, and assessment of minor structural variants such as disulfide-scrambled isomers. Lyophilisation yields a stable, uniform powder.

Regulatory Status & Reference Context

Linaclotide is an approved active ingredient. It was first approved by the US FDA in 2012 and is also approved by the EMA for irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation. As a regulated API, it is normally handled within established CMC frameworks (for example US-DMF Type II dossiers and CTD Module 3 documentation) when used in finished-product submissions such as IND/NDA/ANDA filings.

Research-grade linaclotide supplied for laboratory use is not the approved medicinal product. Nothing on this page is medical advice.

Research supply from Winhycare Pharma

Winhycare Pharma supplies research-grade Linaclotide to research organisations and individual researchers for research and development purposes. Material is supplied at high purity (>99%) under stringent quality control with QC documentation, in secure packaging through global standard logistics, with dedicated technical assistance from our team. We focus on consistent quality and purity, reliable and timely supply, confidential and professional service, and long-term partnerships.

Research use only. Not for human or veterinary use, and not for use in food, drugs, medical devices or cosmetics.

To enquire, tell us the quantity you need, the purity grade, the documentation you require and the destination country. The buyer is responsible for complying with the import and use regulations that apply to Linaclotide in their country.