Product description
Preassembled N-Terminal Functional Tetrapeptide for Semaglutide
Core Functional Tetrapeptide for Efficient Semaglutide Synthesis
The His-Aib-Glu-Gly sequence constitutes the core N-terminal functional domain of Semaglutide. The Aib (α-aminoisobutyric acid) residue, with its gem-dimethyl steric structure, stabilizes the peptide's α-helical conformation, serving as a critical structural modification for high-affinity GLP-1 receptor binding, enhanced enzymatic stability, and prolonged glucose-lowering activity.
Conventional synthesis requires four sequential coupling reactions using individual His, Aib, Glu, and Gly monomers, resulting in low overall yields and increased formation of truncated by-products. This product provides the fully preassembled tetrapeptide, allowing direct incorporation into longer peptide intermediates in a single coupling step. By eliminating three coupling reactions, it significantly reduces impurity formation, shortens production cycles, and serves as a key intermediate for industrial semi-synthetic manufacturing of Semaglutide.
Fully Orthogonal Acid-Labile Protection with One-Step TFA Deprotection
The Boc group at the N-terminus, the Trt group on the histidine side chain, and the OtBu group on glutamic acid are all acid-labile protecting groups that can be removed simultaneously during the final TFA cleavage step, eliminating the need for sequential deprotection. This design is fully compatible with Boc-based liquid-phase fragment synthesis workflows. After assembly of the complete peptide backbone, global deprotection yields the fully unprotected active tetrapeptide, which can then be coupled with the middle and C-terminal peptide fragments to generate full-length Semaglutide.
No Pharmacological or Cosmetic Activity
This molecule contains bulky Boc tert-butyl and Trt triphenylmethyl hydrophobic protecting groups, resulting in a molecular size too large to penetrate cell membranes or the skin barrier. It possesses no intrinsic biological activities such as glucose regulation, collagen stimulation, skin whitening, or soothing effects. Direct injection, oral administration, or topical application may leave residual triphenylmethyl or tert-butyl degradation products, potentially causing skin or mucosal irritation. Therefore, it is not intended for pharmaceutical formulations or cosmetic applications.
Universal Fragment Building Block for Aib-Modified Long-Acting GLP-1 Peptides
In addition to Semaglutide, this intermediate is suitable for the liquid-phase fragment synthesis of various Aib-modified long-acting GLP-1 research peptides and glucose-lowering peptide candidates. The preassembled tetrapeptide greatly simplifies the synthesis of structurally demanding α-helical peptide sequences, reduces purification costs, and serves as a key intermediate for semi-synthetic peptide manufacturing.
This product is supplied exclusively as an industrial intermediate for pharmaceutical API synthesis. It is intended solely for factory-scale liquid-phase peptide fragment synthesis and is not suitable for direct injection, oral administration, or topical application.