Tirzepatide
Also known as LY3298176 · GIP/GLP-1 receptor co-agonist
Tirzepatide is a unimolecular dual agonist engineered on the native glucose-dependent insulinotropic polypeptide (GIP) backbone to activate both the GIP receptor and the GLP-1 receptor - two class-B secretin-family G-protein-coupled receptors.
The overview
What is Tirzepatide?
Tirzepatide is a unimolecular dual agonist engineered on the native glucose-dependent insulinotropic polypeptide (GIP) backbone to activate both the GIP receptor and the GLP-1 receptor - two class-B secretin-family G-protein-coupled receptors. In recombinant-cell assays it engages each receptor's Gs-coupling pathway, activating adenylyl cyclase and raising cyclic AMP, with reported potencies in the sub-nanomolar range (GIPR EC50 ≈ 0.042 nM; GLP-1R EC50 ≈ 0.086 nM). Aib substitutions at positions 2 and 13 confer resistance to dipeptidyl-peptidase-IV cleavage, and a C20 fatty-diacid side chain drives reversible albumin binding that extends plasma residence. The molecule is studied as the reference dual-incretin agonist for receptor-signaling and structure-activity work. Description is mechanistic and in-vitro; no human dosing, therapeutic, or efficacy claim is made.
In the research
Where Tirzepatide shows up
The areas researchers focus on with Tirzepatide - and why it has the science community paying attention.
- Dual GIPR / GLP-1R cAMP-signaling potency assays
- Incretin-receptor structure-activity and DPP-IV-resistance studies
- Albumin-binding pharmacokinetic-extension research
By the numbers
The facts that matter
To the molecule
Molecular specifications
39-residue GIP-based backbone with Aib substitutions at positions 2 and 13 and a C20 fatty-diacid moiety (full sequence per Coskun et al. 2018)Sourced, not claimed
The science behind it
The peer-reviewed studies behind Tirzepatide, linked so you can read them yourself.
- Coskun, T., et al. (2018). 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. Molecular Metabolism.
“LY3298176 is a dual GIP and GLP-1 receptor agonist that potently activates both receptors and improves glycemic control in preclinical models.”
Straight answers
Questions, answered
Is Tirzepatide approved by the FDA?
No. Tirzepatide is not an FDA-approved drug. We supply it as a research-use-only reference compound, identity-verified for purity with a COA on every vial.
What class of compound is Tirzepatide?
Tirzepatide is classified as: Unimolecular dual GIP and GLP-1 receptor agonist (synthetic 39-residue acylated peptide).
What is the molecular weight of Tirzepatide?
The molecular weight of Tirzepatide is 4813.5 g/mol, with a molecular formula of C225H348N48O68.
What is the CAS number for Tirzepatide?
The CAS Registry Number for Tirzepatide is 2023788-19-2.
What is the amino acid sequence of Tirzepatide?
Tirzepatide has the sequence: 39-residue GIP-based backbone with Aib substitutions at positions 2 and 13 and a C20 fatty-diacid moiety (full sequence per Coskun et al. 2018).
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For in-vitro laboratory research use only. Not for human or animal consumption. Bodily introduction into humans or animals is strictly prohibited by law. Tirzepatide is not a drug and is not intended to diagnose, treat, cure, or prevent any disease. These statements have not been evaluated by the FDA.