liraglutide（LYS/CYS)

Liraglutide (LYS/CYS) is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist used for treating type 2 diabetes and, in specific formulations, weight management. It is a modified GLP-1 analogue engineered for once-daily administration. The “LYS/CYS” refers primarily to a specific lysine residue (lysine 26) within the GLP-1 sequence, which is acylated via a glutamic acid spacer to a palmitic acid (C16 fatty acid). This lipidation enhances binding to serum albumin and prolongs half-life, resulting in sustained receptor activation and improved pharmacokinetics compared to native GLP-1.

Appearance:

• Clear, colorless solution for subcutaneous injection.

Source:

• Produced through recombinant DNA technology in Saccharomyces cerevisiae (yeast).

• The GLP-1 analogue is synthetically modified by acylation.

Molecular Weight:

• Approximately 3751.24 Da, higher than unmodified GLP-1 (~4.1 kDa) due to lipid modification.

Structure:

• GLP-1 amino acid sequence with palmitic acid attached via glutamic acid linker to the epsilon-amino group of lysine 26.

• The modification site and linkage chemistry are crucial in defining its properties.

Biological Activity:

• Stimulates insulin secretion in a glucose-dependent manner.

• Suppresses glucagon secretion.

• Slows gastric emptying.

• Reduces appetite, promoting weight loss.

• Binds GLP-1 receptor on pancreatic beta cells and various tissues.

• The lysine acylation affects half-life and duration of action.

Purity and Microbial Contamination:

• Typically ≥95% purity by HPLC.

• Sterility and endotoxin tested to meet pharmaceutical standards.

Identity and Quality Control:

• Mass spectrometry to verify molecular mass and modification.

• Amino acid and peptide mapping confirm sequence and modification.

• HPLC for purity and aggregation.

• Bioactivity assays evaluating receptor activation.

• Immunoassays for GLP-1 receptor binding.

Shelf life and Storage

Applications

• Treatment of type 2 diabetes mellitus.

• Weight management in specific approved formulations.

Key Characteristics

• GLP-1 receptor agonist derived from endogenous peptide.

• Long-acting via lysine 26 palmitoylation using glutamic acid spacer.

• Pharmaceutical-grade sterile injectable.

Citation

• FDA and EMA approval documents for detailed molecule info.

• Clinical trial records via PubMed, clinicaltrials.gov.

• Scientific literature on GLP-1 analogue acylation and long-acting peptide therapeutics.

• Patent databases for structural and manufacturing insights.

• Suggested search keywords: “Liraglutide acylation,” “GLP-1 palmitic acid modification,” “Liraglutide clinical trials,” “GLP-1 receptor binding,” “peptide acylation pharmacokinetics.”