Product description
NHS Active Ester for One-Step Liquid-Phase Conjugation of the Long-Acting Semaglutide Side Chain
The prolonged glucose-lowering activity of Semaglutide is achieved through the C18 stearic acid + γ-Glu + bis-AEEA structure attached at the Lys26 position. The C18 lipid chain reversibly binds to plasma albumin, significantly extending the peptide's circulating half-life, while the bis-AEEA polyether spacer optimizes the balance between lipophilicity and aqueous solubility.
Conventional manufacturing requires sequential activation and coupling steps, often resulting in low coupling efficiency, peptide loss, and multiple by-products. This product features the complete preassembled Semaglutide lipid side chain in the form of an OSu (N-hydroxysuccinimide) active ester, allowing direct liquid-phase conjugation with the free amino group of peptides. By eliminating separate coupling reagent activation steps, it greatly simplifies the modification process, improves conjugation efficiency, and is ideally suited for large-scale industrial liquid-phase post-modification of Semaglutide.
Orthogonal Acid-Labile Protection with Simultaneous tert-Butyl Deprotection
Both terminal carboxyl groups are protected as OtBu tert-butyl esters, ensuring excellent structural stability and minimizing side reactions during liquid-phase coupling. All tert-butyl protecting groups are simultaneously removed during the final TFA cleavage step, producing the fully deprotected, lipid-modified Semaglutide peptide through a unified deprotection process that integrates seamlessly into standard liquid-phase purification workflows.
No Pharmacological or Cosmetic Activity
This molecule contains a long hydrophobic C18 alkyl chain, multiple OtBu tert-butyl ester protecting groups, and a succinimide active ester moiety. Owing to its large molecular size, it cannot penetrate cell membranes or the skin barrier and possesses no intrinsic pharmacological or cosmetic activity, such as glucose regulation, collagen stimulation, skin whitening, or soothing effects. Direct injection, oral administration, or topical application may leave residual tert-butyl ester or succinimide degradation products, potentially causing skin or mucosal irritation. Therefore, it is not intended for pharmaceutical formulations or cosmetic use.
Universal Liquid-Phase Activated Ester for C18 Lipid-Modified Long-Acting GLP Peptides
In addition to Semaglutide, this intermediate is suitable for the liquid-phase side-chain modification of other C18 fatty acid-modified long-acting GLP-1 peptides and long-acting insulin analogs. The preassembled activated lipid side chain effectively addresses the challenges of coupling highly hydrophobic lipid moieties and reduces purification complexity and manufacturing costs, making it an ideal liquid-phase modification intermediate for long-acting GLP peptide development and commercial production.
This product is supplied exclusively as an industrial intermediate for pharmaceutical API synthesis. It is intended solely for liquid-phase peptide modification during pharmaceutical manufacturing and is not suitable for direct injection, oral administration, or topical application.