Tirzepatide

Tirzepatide is a lipidated 39-residue peptide with dual GIP and GLP-1 receptor agonism and a C20 diacid side chain on Lys20.

Identity

Sequence

H-Y[Aib]EGTFTSDYSI[Aib]LDKIAQ[K(γE-2xOEG-C20 diacid)]AFVQWLIAGGPSSGAPPPS-NH2

Residues

39

Molecular formula

C₂₂₅H₃₄₈N₄₈O₆₈

Average molecular weight

4813 g/mol

Monoisotopic mass (calculated)

4810.5249 Da

CAS number

2023788-19-2

PubChem CID

166567236

Strengths

5–100 mg

Other names

LY3298176

Lys20 carries a C20 fatty diacid linked through γ-glutamic acid and two 8-amino-3,6-dioxaoctanoic acid (OEG) units.

Identity data from: PubChem CID 166567236

Research overview

Tirzepatide, also identified as LY3298176, is a 39-residue peptide with an amidated carboxyl terminus. Its sequence includes Aib at positions 2 and 13, together with a modified lysine at position 20 bearing a C20 fatty diacid side chain. That side chain is linked through γ-glutamic acid and two 8-amino-3,6-dioxaoctanoic acid (OEG) units. The discovery publication describes the compound as a fatty-acid-modified peptide with agonist activity at both GIP and GLP-1 receptors [1].

The discovery work used signalling and functional assays in cell lines expressing recombinant or endogenous incretin receptors. The subsequent signalling study examined relative activity at GIP and GLP-1 receptors and described a method for calculating occupancy of each receptor. Its analysis reported a greater degree of engagement at the GIP receptor than at the GLP-1 receptor. The same study also included experiments in primary islets to examine the role of β-arrestin1 [1][2].

At the GLP-1 receptor, the later study found a signalling preference for cAMP generation over β-arrestin recruitment, together with weaker receptor internalization than with GLP-1. At the GIP receptor, the reported signalling pattern resembled that of native GIP. The reported pharmacological comparisons used native GIP at the GIP receptor and GLP-1 at the GLP-1 receptor as reference ligands for the signalling measurements [2].

Laboratory storage and handling

Store the sealed vial at the temperature specified in the lot documentation, protected from light and moisture. Allow the closed vial to reach room temperature before opening to limit condensation on the material. Avoid repeated freezing and thawing of laboratory stocks. Record the lot identifier and storage history with the experiment, and use standard laboratory protective equipment when handling the peptide.

Questions about Tirzepatide

References

1. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept. Mol Metab 2018. PMID 30473097
2. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight 2020. PMID 32730231

Identity data checked on 2026-09-24. Literature summaries describe published research models and are not specifications of any product lot.