Tirzepatide
⚠ For in-vitro research use only. Not for human consumption. Not FDA approved.
Tirzepatide is a synthetic 39-amino acid peptide engineered from the native GIP sequence with incorporated GLP-1 receptor activity. It is the first dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist — a class referred to in the literature as a "twincretin."
The compound features two non-coded α-aminoisobutyric acid (Aib) residues at positions 2 and 13 that confer resistance to DPP-4 enzymatic degradation, and a C20 fatty diacid moiety conjugated to Lys20 via a γGlu-2×OEG linker, enabling extended plasma half-life through albumin binding (~5 days). The C-terminus is amidated.
Research Applications
- Dual incretin receptor signaling and downstream pathway analysis (GIP/GLP-1)
- In-vitro models of glucose-dependent insulin secretion and glucagon suppression
- Metabolic pathway research involving lipid metabolism and energy homeostasis
- Receptor binding affinity and selectivity studies (GIPR vs. GLP-1R)
- Structural biology and cryo-EM investigations of peptide–receptor complexes
Published Research Context
Tirzepatide has been the subject of extensive preclinical and structural research. Cryo-EM studies (Sun et al., 2022) have resolved the peptide bound to both GLP-1R and GIPR in complex with G-proteins, revealing distinct interaction networks including ionic bonds, hydrogen bonding, and hydrophobic contacts at the receptor interfaces. The compound's 14 unique amino acid substitutions (relative to native GLP-1) and its dual receptor engagement mechanism make it a significant tool for studying multiplexed pharmacological signaling.
Specifications
- Molecular Formula: C225H348N48O68
- Molecular Weight: 4,813.53 g/mol
- Sequence Length: 39 amino acids
- CAS Number: 2023788-19-2
- Form: White lyophilized powder
- Storage: Lyophilized, −20°C, protected from light
- Purity: ≥98% by HPLC
⚠ For in-vitro research use only. Not for human consumption. Not FDA approved. Certificate of Analysis included with every order.
🔬 Research Reference: Tirzepatide — Compound Reference & Research Data | Certificate of Analysis (Lot 2603)