Buy Tirzepatide in Canada — 20mg & 60mg Research Vials, Lab-Tested

What tirzepatide is

Tirzepatide (development code LY3298176) is a fatty-acid-modified synthetic peptide that activates two incretin receptors, the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R)^[1]. Unlike most research peptides sold in Canada, it is also an approved prescription medicine: Eli Lilly markets it as Mounjaro and Zepbound, and both brand names appear in the Health Canada Drug Product Database as prescription products. The vials on this page are research-grade material; they are not Mounjaro or Zepbound, not a licensed medicine, and are sold for laboratory research only.

Key facts

• Identity: C₂₂₅H₃₄₈N₄₈O₆₈, 4813 g/mol (PubChem CID 166567236); CAS 2023788-19-2; ChEMBL4297839.
• Target profile: dual agonist, weighted toward the GIP receptor and biased toward cAMP signalling at the GLP-1 receptor in cell studies^[2].
• Regulatory status: approved by the US FDA in May 2022 for type 2 diabetes^[12] and in 2023, as Zepbound, for chronic weight management^[14]; a 2024 review lists approval for type 2 diabetes in the USA, EU, Japan and other countries^[13]. In Canada, Mounjaro and Zepbound are listed as prescription drugs in the Drug Product Database.
• Evidence base: cell pharmacology, mouse studies and a large phase 3 clinical programme (SURPASS in type 2 diabetes, SURMOUNT in obesity)^{[7, 9]}.
• Batch documentation on this site: no batch-specific COA for the 20mg or 60mg vial is posted in the COA library at the time of writing.

Discovery and development

Lilly scientists described LY3298176 in 2018 as a peptide built to test whether adding GIP-receptor activity to GLP-1-receptor agonism would add metabolic effect in type 2 diabetes. The discovery paper characterised it in cell lines expressing recombinant or native incretin receptors and in mice, where it drove glucose-dependent insulin secretion through both receptors, and reported the first randomised phase 1 studies in healthy volunteers and people with type 2 diabetes, whose primary aim was safety and tolerability^[1]. A 26-week phase 2 study in type 2 diabetes followed, comparing several dose levels with placebo and with the GLP-1 receptor agonist dulaglutide^[6]. Phase 3 began with SURPASS-1, a 40-week placebo-controlled trial at 52 centres in India, Japan, Mexico and the USA in people whose diabetes was not controlled by diet and exercise^[7].

Identity

Mechanisms studied, by model

Receptor pharmacology in cells

Occupancy calculations in a 2020 study showed tirzepatide engaging the GIP receptor more than the GLP-1 receptor at clinically relevant exposure, which the authors called an “imbalanced” mechanism. At the GIP receptor it behaved like native GIP; at the GLP-1 receptor it favoured cAMP generation over β-arrestin recruitment and internalised the receptor less than GLP-1 did. In primary islets, β-arrestin1 limited the insulin response to GLP-1 but not to GIP or tirzepatide^[2]. A separate HEK293 study also found bias for tirzepatide, measured this time as ERK1/2 phosphorylation relative to cAMP at both receptors^[3], a reminder that “bias” depends on which pathways are compared.

Structure

Cryo-electron microscopy and molecular-dynamics work in 2022 resolved how tirzepatide sits in each receptor: it activates GIPR much as GIP does but engages GLP-1R differently from GLP-1, with less receptor desensitisation, and the fatty-acid modification together with the amino-acid sequence shapes that behaviour^[4].

Mouse studies

In obese mice, tirzepatide improved insulin sensitivity more than a GLP-1 receptor agonist. In mice lacking the GLP-1 receptor, where no GLP-1R-driven weight change could occur, it still improved insulin sensitivity through glucose disposal in white adipose tissue, and a long-acting GIP-receptor agonist did the same, pointing to GIPR signalling for that effect^[5]. The 2018 discovery paper had already shown that its insulin-secretion effect in mice required both receptors^[1].

The clinical programme, described by design

Tirzepatide is one of the few compounds in this catalogue with large human trials. They are summarised here by design and endpoint only; this page does not report or claim clinical outcomes for the research material sold here, and gives no dosing or administration information.

• SURPASS-1 (2021): 40-week, double-blind, placebo-controlled phase 3 monotherapy trial in type 2 diabetes^[7].
• SURPASS-2 (2021): 40-week open-label phase 3 comparison with semaglutide in 1,879 people with type 2 diabetes; primary endpoint glycated haemoglobin^[8].
• SURMOUNT-1 (2022): 72-week phase 3 trial in 2,539 adults with obesity or overweight with a weight-related complication, excluding diabetes; the co-primary endpoints concerned body weight^[9].
• SURMOUNT-OSA (2024): two 52-week phase 3 trials in adults with moderate-to-severe obstructive sleep apnea and obesity, one with and one without positive-airway-pressure therapy; primary endpoint the apnea–hypopnea index^[10].
• SUMMIT (2025): 731 patients with heart failure with preserved ejection fraction and obesity; primary endpoints a cardiovascular-death/heart-failure composite and a quality-of-life score^[11].

On safety, a 2023 meta-analysis of ten trials (6,836 participants) found gastrointestinal adverse events, mainly nausea and diarrhoea, to be the most common and dose-dependent, with severe hypoglycaemia, pancreatitis and gallbladder events rare^[12].

Study summary

What the evidence does not show

• The clinical trials used Lilly’s manufactured medicine under trial protocols. They say nothing about the identity, purity or content of research-grade vials from any supplier, including these.
• Regulatory approval of Mounjaro and Zepbound does not extend to research-grade tirzepatide. This material is not a substitute for a prescription medicine.
• Receptor “bias” findings depend on the assay: one study reported cAMP-over-β-arrestin bias at GLP-1R^[2], another reported ERK1/2-over-cAMP bias at both receptors^[3].
• The GIPR-driven insulin-sensitising effect was shown in mice^[5]; how far it explains findings in people is not settled by that work.
• No study of any SPO batch exists, and no batch COA for these vials is posted yet.

Handling and storage

Both listings are lyophilized powder in sealed vials. Keep unopened vials frozen at −20 °C, dry and protected from light, and avoid repeated freeze–thaw cycles. Bacteriostatic water is listed separately; solvent, concentration and method are set by the researcher. Note the batch number on the label so it can be matched to any report later posted in the COA library.

References

1. Coskun T, Sloop KW, Loghin C 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 18:3-14. doi:10.1016/j.molmet.2018.09.009. PMID 30473097
2. Willard FS, Douros JD, Gabe MB et al. (2020). Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI insight 5(17). doi:10.1172/jci.insight.140532. PMID 32730231
3. Yuliantie E, Darbalaei S, Dai A et al. (2020). Pharmacological characterization of mono-, dual- and tri-peptidic agonists at GIP and GLP-1 receptors. Biochemical pharmacology 177:114001. doi:10.1016/j.bcp.2020.114001. PMID 32360365
4. Sun B, Willard FS, Feng D et al. (2022). Structural determinants of dual incretin receptor agonism by tirzepatide. Proceedings of the National Academy of Sciences of the United States of America 119(13):e2116506119. doi:10.1073/pnas.2116506119. PMID 35333651
5. Samms RJ, Christe ME, Collins KA et al. (2021). GIPR agonism mediates weight-independent insulin sensitization by tirzepatide in obese mice. The Journal of clinical investigation 131(12). doi:10.1172/JCI146353. PMID 34003802
6. Frias JP, Nauck MA, Van J et al. (2018). Efficacy and safety of LY3298176, a novel dual GIP and GLP-1 receptor agonist, in patients with type 2 diabetes: a randomised, placebo-controlled and active comparator-controlled phase 2 trial. Lancet (London, England) 392(10160):2180-2193. doi:10.1016/S0140-6736(18)32260-8. PMID 30293770
7. Rosenstock J, Wysham C, Frías JP et al. (2021). Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial. Lancet (London, England) 398(10295):143-155. doi:10.1016/S0140-6736(21)01324-6. PMID 34186022
8. Frías JP, Davies MJ, Rosenstock J et al. (2021). Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. The New England journal of medicine 385(6):503-515. doi:10.1056/NEJMoa2107519. PMID 34170647
9. Jastreboff AM, Aronne LJ, Ahmad NN et al. (2022). Tirzepatide Once Weekly for the Treatment of Obesity. The New England journal of medicine 387(3):205-216. doi:10.1056/NEJMoa2206038. PMID 35658024
10. Malhotra A, Grunstein RR, Fietze I et al. (2024). Tirzepatide for the Treatment of Obstructive Sleep Apnea and Obesity. The New England journal of medicine 391(13):1193-1205. doi:10.1056/NEJMoa2404881. PMID 38912654
11. Packer M, Zile MR, Kramer CM et al. (2025). Tirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity. The New England journal of medicine 392(5):427-437. doi:10.1056/NEJMoa2410027. PMID 39555826
12. Mishra R, Raj R, Elshimy G et al. (2023). Adverse Events Related to Tirzepatide. Journal of the Endocrine Society 7(4):bvad016. doi:10.1210/jendso/bvad016. PMID 36789109
13. France NL, Syed YY (2024). Tirzepatide: A Review in Type 2 Diabetes. Drugs 84(2):227-238. doi:10.1007/s40265-023-01992-4. PMID 38388874
14. Abbasi J (2023). FDA Green-Lights Tirzepatide, Marketed as Zepbound, for Chronic Weight Management. JAMA 330(22):2143-2144. doi:10.1001/jama.2023.24539. PMID 37966831