Tirzepatide
Also known as LY3298176
Tirzepatide is a synthetic peptide that activates both the GIP and GLP-1 receptors. Researchers study it to understand how combined incretin receptor signaling affects glucose control, body weight, and related metabolic outcomes.
Approved drug substance
Size
10 options- Catalog no.
- TR5
- Specification
- 5mg *10vials
- Per kit
- 10 vials
For laboratory research use only. Not for human or animal consumption. Buyers must be 21 or older.
Overview
Tirzepatide was developed by Eli Lilly under the code LY3298176. It is a 39-amino-acid linear peptide built largely on the sequence of native GIP, with a C20 fatty diacid side chain that binds albumin and extends its half-life. It is approved in the United States and other regions for type 2 diabetes and chronic weight management. The SURPASS program studied it in type 2 diabetes, and the SURMOUNT program studied it in obesity. Further trials have examined obstructive sleep apnea, heart failure, and liver fat.
Class: Dual GIP and GLP-1 receptor agonist
Mechanism of action
How the compound acts, as described in the literature.
Activates the GIP receptor with potency similar to native GIP and the GLP-1 receptor with lower potency than native GLP-1, an imbalanced profile that favors GIP receptor signaling.
At the GLP-1 receptor it favors cAMP signaling over beta-arrestin recruitment, a bias that cell studies link to reduced receptor internalization.
Both receptor actions increase glucose-dependent insulin secretion from pancreatic beta cells. Clinical studies have also reported lower glucagon levels and improved insulin sensitivity.
Reduces food intake and body weight through central appetite pathways. In mice, its weight and food-intake effects exceeded those of a selective GLP-1 receptor agonist.
Published research
Selected studies, each linked to its PubMed record. Summaries describe what the studies reported.
2022
Phase 3 RCT
PMID 35658024Tirzepatide Once Weekly for the Treatment of Obesity.
Jastreboff AM, et al. · N Engl J Med
SURMOUNT-1 randomized 2,539 adults with obesity without diabetes for 72 weeks. Mean body-weight reductions were 15.0% to 20.9% across three dose levels versus 3.1% with placebo.
2021
Phase 3 RCT
PMID 34170647Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes.
Frías JP, et al. · N Engl J Med
SURPASS-2 compared tirzepatide with semaglutide in 1,879 adults with type 2 diabetes over 40 weeks. All three tirzepatide dose levels lowered HbA1c and body weight more than the semaglutide comparator.
2018
Discovery and phase 1 study
PMID 30473097LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.
Coskun T, et al. · Mol Metab
Described the discovery of LY3298176. In mice it improved glucose tolerance through both receptors and reduced food intake and body weight more than a GLP-1 receptor agonist; phase 1 data in type 2 diabetes showed lower fasting glucose.
Evidence & safety
What the research does not show, and the adverse events and regulatory status it reports.
Gastrointestinal adverse events were the most common in SURMOUNT-1, mostly mild to moderate and concentrated during dose escalation, and adverse events led to discontinuation in 4.3% to 7.1% of tirzepatide groups versus 2.6% with placebo. US labeling carries a boxed warning based on thyroid C-cell tumors seen in rodents, along with warnings for pancreatitis and gallbladder disease. Most pivotal trials were sponsor-funded.
Specifications
All sizes, exactly as catalogued.
| Catalog no. | Product | Specification | Vials per kit |
|---|---|---|---|
| TR5 | Tirzepatide | 5mg *10vials | 10 |
| TR10 | Tirzepatide | 10mg *10vials | 10 |
| TR15 | Tirzepatide | 15mg *10vials | 10 |
| TR20 | Tirzepatide | 20mg *10vials | 10 |
| TR30 | Tirzepatide | 30mg *10vials | 10 |
| TR40 | Tirzepatide | 40mg *10vials | 10 |
| TR45 | Tirzepatide | 45mg *10vials | 10 |
| TR50 | Tirzepatide | 50mg *10vials | 10 |
| TR60 | Tirzepatide | 60mg *10vials | 10 |
| TR100 | Tirzepatide | 100mg *10vials | 10 |
For laboratory research use only. Not for human or animal consumption. Not intended to diagnose, treat, cure or prevent any disease. Research summaries are provided for educational purposes and do not describe this product’s use.