Product description
Trt-Protected His-Aib Core Dipeptide for Semaglutide Synthesis
A Trt-Protected Solution to Histidine Synthesis Challenges
The imidazole ring of unprotected histidine is highly basic and prone to cyclization, cross-linking, and the formation of truncated by-products during peptide synthesis. This product employs a triphenylmethyl (Trt) protecting group to completely shield the imidazole ring through steric hindrance, ensuring clean solid-phase coupling with minimal side reactions. The fully preassembled His-Aib dipeptide can be incorporated into the resin in a single coupling step, eliminating one coupling reaction compared with sequential incorporation of His and Aib monomers. This significantly reduces truncated impurities and improves manufacturing efficiency for large-scale industrial solid-phase synthesis of Semaglutide.
The Aib (α-aminoisobutyric acid) residue, with its gem-dimethyl structure, promotes the formation of a stable α-helical conformation, serving as a critical structural modification for high-affinity GLP-1 receptor binding and prolonged glucose-lowering activity.
Orthogonal Stepwise Deprotection Compatible with Standard Fmoc SPPS
The N-terminal Fmoc protecting group can be selectively removed under mild piperidine treatment without affecting the growing peptide chain. The Trt protecting group on the histidine side chain remains intact throughout peptide assembly and is removed only during the final TFA cleavage, making the product fully compatible with standard Fmoc solid-phase peptide synthesis (SPPS) workflows. After global deprotection, the native His-Aib dipeptide is obtained and can be further elongated through coupling with Glu, Gly, and additional N-terminal residues.
No Pharmacological or Cosmetic Activity
This intermediate contains bulky hydrophobic Fmoc fluorenyl and Trt triphenylmethyl protecting groups, resulting in a molecular structure 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 aromatic protecting-group degradation products that could cause skin or mucosal irritation. Therefore, it is not intended for pharmaceutical formulations or cosmetic applications.
Universal Preassembled Building Block for His-Aib-Containing Long-Acting GLP Peptides
In addition to Semaglutide, this intermediate is suitable for the solid-phase synthesis of a wide range of Aib-modified long-acting GLP-1 research peptides and glucose-lowering peptide candidates. Trt-protected His-Aib is an essential high-purity building block for the synthesis of long-chain GLP peptides, significantly reducing purification complexity and production costs associated with histidine-containing sequences.
This product is supplied exclusively as an industrial intermediate for pharmaceutical API synthesis. It is intended solely for factory-scale solid-phase peptide synthesis and is not suitable for direct injection, oral administration, or topical application.