semaglutide（LYS/CYS)

Semaglutide (LYS/CYS) is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist designed for once-weekly treatment of type 2 diabetes and for weight management. It is a modified GLP-1 analogue with specific acylation at lysine (LYS) and cysteine (CYS) residues, typically involving attachment of a C18 fatty diacid. This modification extends half-life by enhancing binding to albumin and slowing clearance, resulting in sustained GLP-1 receptor activation.

Appearance:

• White to off-white solid powder or lyophilized solid; forms clear, colorless solution after reconstitution.

Source:

•  Synthesized chemically via peptide synthesis; not naturally derived.

Molecular Weight:

• Approximately 4113 Da, higher than unmodified GLP-1 (~4.1 kDa) due to lipid modification.

Structure:

• GLP-1 peptide backbone modified at specific LYS and CYS residues with fatty acid moiety; exact sites and linkage chemistry are proprietary.

Biological Activity:

• Stimulates glucose-dependent insulin secretion

• Suppresses glucagon secretion

• Slows gastric emptying

• Reduces appetite, promoting weight loss

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

Purity and Microbial Contamination:

• Purity ≥95% confirmed by HPLC

• Sterility and endotoxin within strict pharmaceutical limits

Identity and Quality Control:

• MS confirms molecular weight and modifications

• Amino acid analysis and peptide mapping verify sequence and modifications

• HPLC and SDS-PAGE assess purity and aggregation

• Bioactivity assays test receptor activation in vitro

• Immunochemical assays measure receptor binding affinity

Shelf life and Storage

Applications:

• Treatment of type 2 diabetes and weight management.

Key Characteristics:

• GLP-1 receptor agonist with extended half-life

• Modified at lysine and cysteine for lipidation

• Pharmaceutical-grade sterile lyophilisate for injection

Citation

• FDA and EMA approval documents

• Clinical trial databases (PubMed, clinicaltrials.gov)

• Publications on PEGylation and acylation of peptides

• Patents on semaglutide structure and synthesis

• Keywords: “Semaglutide mechanism of action,” “acylated GLP-1 structure,” “Semaglutide clinical trials,” “GLP-1 receptor binding,” “peptide acylation”