Semaglutide

Semaglutide

Price range: $50.00 through $100.00

GLP-1 Receptor Agonist · 31-Amino-Acid Lipidated Peptide

Semaglutide is a synthetic 31-amino-acid analog of human glucagon-like peptide-1 (GLP-1). Engineered for extended half-life and enzymatic stability, it incorporates an α-aminoisobutyric acid (Aib) substitution at position 8 alongside a C₁₈ fatty-diacid side chain conjugated to Lys²⁶ via a hydrophilic γGlu-2×OEG spacer. This structural modification facilitates tight, reversible binding to serum albumin, extending its circulating plasma half-life to approximately 7 days. Large-scale trial programs (SUSTAIN, STEP, PIONEER; Wilding et al., 2021) have extensively characterized its selective GLP-1 receptor agonism, glucose-dependent insulinotropic signaling, delay of gastric emptying, and central energy-balance regulation.

Supplied at 10mg, 20mg and 30mg.

SKU: SEMA-PARENT Categories: ,

Description

Overview

Semaglutide is a synthetic 31-amino-acid peptide analog of human glucagon-like peptide-1 (GLP-1). Designed to overcome the ultra-short terminal half-life of native GLP-1, Semaglutide incorporates an α-aminoisobutyric acid (Aib) substitution at position 8 to prevent enzymatic breakdown alongside a lipidated side chain at position 26.

The addition of a C₁₈ fatty-diacid chain via a hydrophilic γGlu-2×OEG spacer enables non-covalent binding to circulating serum albumin, yielding a prolonged elimination half-life of approximately 7 days in vivo.

Key Technical Specifications

Sequence HXEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
(X = Aib; Lys26 conjugated to γGlu-2×OEG-C18 diacid)
Molecular Formula C₁₈₇H₂₉₁N₄₅O₅₉
Molecular Weight ~4113.58 g/mol
CAS Number 910463-68-2
Elimination Half-Life ~7 days (in vivo, human)
Solubility Bacteriostatic Water / Sterile Water
Primary Class Selective GLP-1 Receptor Agonist

Biochemical Architecture & Mechanisms

1. Enzymatic Resistance via Aib&sup8; Substitution

Native GLP-1 undergoes rapid cleavage by Dipeptidyl Peptidase IV (DPP-IV) at the N-terminus. Replacing L-alanine with non-canonical α-aminoisobutyric acid (Aib) at position 8 confers conformational stability and resistance to DPP-IV digestion.

2. Extended Plasma Residence & Linker Chemistry

The acylation at Lys²⁶ uses a specialized spacer consisting of a glutamic acid residue and two 8-amino-3,6-dioxaoctanoic acid (OEG) units attached to a C₁₈ fatty-diacid. This combination provides high affinity for human serum albumin without obscuring key receptor-binding residues.

3. Receptor Agonism & Downstream Signaling

  • Insulinotropic Signaling: Activates GLP-1 receptors on pancreatic beta cells to induce glucose-dependent insulin secretion.
  • Central & Peripheral Regulation: Modulates central nervous system satiety centers and delays gastric emptying rates in research models.

Trial Program Literature: Semaglutide has been extensively documented in clinical research literature—including the SUSTAIN, STEP, and PIONEER trial series (Wilding et al., 2021)—focusing on GLP-1R kinetics, metabolic signaling, and hepatic lipid management.

For laboratory research, educational, and analytical reference only. Strictly not for human or veterinary use.

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