Also known as: LY3298176
A synthetic peptide that activates two incretin hormone receptors, GIP and GLP-1, in one molecule. It has a large body of published phase 3 human trials and a growing set of rodent and cell studies.
Tirzepatide is a single peptide that activates both the GIP receptor and the GLP-1 receptor [1]. In human fat cells and mice, long-acting GIP-receptor activation increased insulin signaling and glucose uptake in the presence of insulin and increased lipolysis markers without it, suggesting different roles in fed and fasted states [2]. A 2025 preprint proposes that tirzepatide also amplifies leptin signaling in hypothalamic POMC neurons in mice; this has not yet been peer reviewed [6].
| Study | Model | Reported result | Source |
|---|---|---|---|
| GIP receptor and adipocytes [2] | Mouse Human adipocyte cultures and high-fat-diet mice | Researchers measured insulin signaling, glucose uptake and lipolysis; in mice, circulating triglycerides fell during a lipid challenge and fat-tissue fatty-acid uptake rose | Peer-reviewed Cell Metab 2024 |
| Liver lipid study (Li et al.) [3] | Mouse High-fat and high-fat/fructose/cholesterol diet models, 12 weeks, n=5 per group | Researchers reported body/liver weight, glucose and liver-lipid measurements vs untreated diet-fed mice; liver CD36 and OBP2A expression was lower. | Peer-reviewed Genes Dis 2025 |
| Liver and HepG2 study (Wu et al.) [4] | Mouse High-fat diet model, 16 weeks total, n=7 per group; plus palmitate-loaded HepG2 cells | Lower liver weight and histology scores; lower triglyceride and cholesterol in cells. Paper reports conflicting AMPK/NF-κB directions between sections | Peer-reviewed Am J Transl Res 2025 |
| Kidney and gut microbiome [5] | Mouse db/db mouse kidney model, 8 weeks, n=6 per group, with antibiotic-depleted comparison group | Measured glucose, HbA1c, lipids, serum creatinine and urine albumin/creatinine; reported shifts in gut genera that correlated with kidney markers | Peer-reviewed Front Mol Biosci 2025 |
| Leptin combination (preprint) [6] | Mouse High-fat-diet model | Combination with leptin increased POMC neuron firing and brown-fat thermogenic gene expression vs either alone; no numbers in abstract | Company-reported bioRxiv 2025 |
Human trials are listed for research context only; outcomes are reported in the linked publications. Animal and lab results do not establish effects in humans.
PureLab does not supply this compound. This page summarizes published research only.