Tirzepatide
Tirzepatide is a synthetic 39-residue peptide that functions as a dual agonist of the GIP (gastric inhibitory polypeptide) and GLP-1 (glucagon-like peptide-1) receptors, two class B G-protein-coupled receptors. It is supplied as a reference material strictly for in-vitro laboratory research.
View product · from $165What it is
Tirzepatide (research designation LY3298176) is a single-chain, linear 39-amino-acid synthetic peptide derived from the GIP scaffold and engineered to engage two class B G-protein-coupled receptors. Its primary structure incorporates two 2-aminoisobutyric acid (Aib) residues at positions 2 and 13, a C-terminal amide, and a lysine at position 20 that is conjugated through a γ-glutamate and two 8-amino-3,6-dioxaoctanoic acid (AEEA) spacers to a C20 fatty diacid (1,20-eicosanedioic acid). The Aib substitutions and the lipidated linker are structural features studied for their influence on conformational stability, protease resistance, and albumin association in biochemical assays. The molecule carries the molecular formula C225H348N48O68 and a monomeric molecular weight of approximately 4813.45 Da.
Mechanism (in-vitro research context)
In receptor-binding and cell-based reporter assays, tirzepatide binds and activates both the GIP receptor (GIPR) and the GLP-1 receptor (GLP-1R), two class B (secretin-family) G-protein-coupled receptors. Receptor engagement in vitro couples to Gs-mediated stimulation of adenylate cyclase and accumulation of cyclic AMP, which is the principal readout used to quantify agonist potency and efficacy in these assay systems. Published in-vitro pharmacology characterizes the molecule as an imbalanced and biased dual agonist, with relatively greater activity at GIPR than at GLP-1R and differential recruitment of downstream effectors such as β-arrestin. These properties make it a frequent tool compound for comparative class B GPCR signaling, receptor-selectivity, and structure-activity studies.
Research areas
- GIP receptor (GIPR) binding and cAMP accumulation assays
- GLP-1 receptor (GLP-1R) binding and functional activation assays
- Class B GPCR signaling bias and β-arrestin recruitment studies
- Receptor selectivity and dual-agonist structure-activity relationship (SAR) profiling
- Cryo-EM and structural biology of peptide-receptor complexes
- Comparative class B GPCR pharmacology with reference agonists
Chemistry
- Molecular weight
- 4813.45 Da
- CAS
- 2023788-19-2
- Formula
- C225H348N48O68
- Sequence
- YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS-NH2 (X = 2-aminoisobutyric acid at positions 2 and 13; C-terminal amide; Lys20 conjugated via γ-Glu and two AEEA spacers to a C20 fatty diacid)
Laboratory handling
Typically supplied as a lyophilized powder for laboratory use. The dry solid is generally stored desiccated and protected from light, commonly at -20 C or colder for long-term storage. Reconstituted stock solutions are handled cold, aliquoted to minimize repeated freeze-thaw cycles, and used promptly to limit aggregation and hydrolytic degradation. Analytical identity and stability are routinely monitored by reversed-phase HPLC and mass spectrometry. All handling is for in-vitro research purposes only.
FAQ
What is the amino acid sequence of tirzepatide?
It is a 39-residue linear peptide on a GIP-based scaffold (YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS-NH2), where X denotes 2-aminoisobutyric acid (Aib) at positions 2 and 13, with a C-terminal amide and a lysine at position 20 conjugated through a γ-Glu and two AEEA spacers to a C20 fatty diacid.
What is the molecular weight and molecular formula?
The molecular formula is C225H348N48O68, corresponding to a monomeric molecular weight of approximately 4813.45 Da.
How is identity and purity verified in the laboratory?
Identity is typically confirmed by mass spectrometry (observed mass versus theoretical 4813.45 Da) and purity is assessed by reversed-phase HPLC, often reported as area-percent at a defined wavelength.
What receptors does it engage in vitro?
In receptor-binding and cell-based reporter assays it activates both the GIP receptor (GIPR) and the GLP-1 receptor (GLP-1R), two class B G-protein-coupled receptors, with cAMP accumulation as a common functional readout.
How should it be stored in the lab?
The lyophilized powder is generally kept desiccated, protected from light, and stored at -20 C or colder; reconstituted solutions are aliquoted and kept cold to minimize freeze-thaw cycles and hydrolytic degradation.
References
- Coskun T. et al. (2018) LY3298176, a novel dual GIP and GLP-1 receptor agonist. Molecular Metabolism 18:3-14.
- Willard F.S. et al. (2020) Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight 5(17):e140532.
- PubChem Compound Summary, CID 156588324 (Tirzepatide).
For laboratory research use only. Not for human or veterinary use. Not for diagnostic or therapeutic use. These products have not been approved or evaluated by the U.S. Food and Drug Administration. No statement on this site has been evaluated by the FDA. These products are not intended to diagnose, treat, cure, mitigate, or prevent any disease, and are not intended for human or veterinary use. See our research-use terms and terms of service.