What is tirzepatide?
Tirzepatide is a single peptide that activates the receptors for both gut incretin hormones, GIP and GLP-1. Here is how it works, how it was developed, and what research has reported.
At a glance
- Class
- Dual GIP / GLP-1 receptor agonist
- Development code
- LY3298176 1
- Structure
- 39-amino-acid synthetic peptide with a C20 fatty diacid side chain
- Molecular formula
- C225H348N48O68
- Molecular weight
- ≈ 4813.5 g/mol
- Appearance
- White lyophilized powder
- Our fill size
- 30mg
Two incretins, one molecule
Incretins are hormones released by the gut after eating that boost insulin secretion when blood glucose is high. There are two: GLP-1 and GIP. GLP-1 also slows stomach emptying and signals fullness; GIP acts on the pancreas and on fat tissue.
Tirzepatide was designed to test whether adding GIP activity improves on the benefits already seen with GLP-1 receptor agonists.1 It is a fatty-acid-modified peptide: the fatty side chain lets it bind albumin in the blood, which slows its clearance and gave it a profile suited to once-weekly dosing.1
How it was developed
Eli Lilly developed tirzepatide under the code LY3298176. Its 2018 discovery paper characterised it in cell lines expressing the incretin receptors, then in mice (body weight, food intake, insulin secretion and glucose profiles), and then in early human studies: single and multiple ascending-dose studies in healthy volunteers and a four-week study in people with type 2 diabetes, using the GLP-1 drug dulaglutide as a comparator.1
What clinical research has reported
In the SURMOUNT-1 trial, 2,539 adults with obesity, or with overweight plus a weight-related condition and without diabetes, received weekly tirzepatide or placebo for 72 weeks. Mean body weight fell by 15.0%, 19.5% and 20.9% at the three doses tested, compared with 3.1% with placebo. Side effects were mostly gastrointestinal, mild to moderate, and occurred mainly while the dose was being increased.2
Tirzepatide is now an approved medicine: the FDA approved it for type 2 diabetes in 2022 (as Mounjaro) and for chronic weight management in 2023 (as Zepbound). Those approvals cover the pharmaceutical product prescribed under medical supervision.
Clinical results describe the approved medicine. Research-grade tirzepatide is supplied for laboratory work only.
Where tirzepatide is used in the lab
In laboratory and preclinical research, tirzepatide is used to study glucose control, insulin secretion, food intake and fat-tissue biology, and as the dual-agonist reference point between single GLP-1 agonists and triple agonists such as GLP-3RT. Our GLP-3RT overview explains what adding the glucagon receptor changes.
Handling tirzepatide in the lab
Lyophilized tirzepatide is stable stored frozen at −4 °F and protected from light. Let a vial reach room temperature before opening, reconstitute with bacteriostatic water added slowly down the side of the vial, swirl rather than shake, and keep the solution refrigerated at 36–46 °F.
Before using any lot, check its certificate of analysis. Our current tirzepatide lot, VD-TZ30-2610, tested at 99.40% purity by HPLC with identity confirmed by LC-MS at VeriPure Labs. View the certificate ↗ or see every lot on our lab reports page.
Frequently asked questions
What is the difference between tirzepatide and GLP-3RT?
Tirzepatide activates the GIP and GLP-1 receptors. GLP-3RT also activates the glucagon receptor, making it a triple agonist.
Is tirzepatide the same as Mounjaro or Zepbound?
Mounjaro and Zepbound are the brand names of the approved medicines, whose active ingredient is tirzepatide. Research-grade tirzepatide is a laboratory reagent, not those medicines.
Why does tirzepatide last so long?
A C20 fatty diacid side chain lets it bind albumin in the blood, which slows its clearance and supports once-weekly dosing in clinical use.
Is research tirzepatide for human use?
No. Vivid DNA supplies tirzepatide strictly for laboratory research. It is not a drug, food or supplement, and is not for human or veterinary use.
References
- Coskun T, Sloop KW, Loghin C, et al. 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. 2018;18:3–14. PubMed 30473097 ↗
- Jastreboff AM, Aronne LJ, Ahmad NN, et al. Tirzepatide once weekly for the treatment of obesity. New England Journal of Medicine. 2022;387(3):205–216. doi:10.1056/NEJMoa2206038 ↗
More research overviews
Research use only. Vivid DNA products are sold strictly for laboratory research. They are not drugs, foods, cosmetics or supplements, are not for human or veterinary use, and are not intended to diagnose, treat, cure or prevent any disease. Clinical results described here refer to investigational or approved medicines studied under medical supervision, not to research-grade material. This article summarises published research and has not been evaluated by the Food and Drug Administration.