Tirzepatide (10 Vial Box)

Compliance & Disclaimer

• For Research Use Only
• Not FDA or EMA approved for clinical application
• Evidence is limited to preclinical studies; safety and efficacy in humans remain unestablished.

Tirzepatide is a synthetic peptide classified as a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor, representing a novel approach within the incretin-based research paradigm. Mechanistically, Tirzepatide binds to and activates both receptors, enabling investigation into combined incretin signaling and its impact on metabolic regulation. Structural studies reveal that Tirzepatide adopts an α-helical conformation similar to native incretins, with receptor interactions that confer biased signaling toward cyclic AMP pathways at the GLP-1 receptor, a property hypothesized to influence glycemic control and body weight regulation. [nature.com] [pnas.org]

Preclinical and clinical research has examined Tirzepatide’s pharmacodynamics, including its effects on insulin secretion, glucagon modulation, and gastric motility under controlled experimental conditions. Investigations in human islets demonstrate that Tirzepatide stimulates hormone secretion through both incretin receptors, supporting its role as a model compound for studying dual-receptor agonism. Additional studies have explored its pharmacokinetic profile, noting albumin binding and extended half-life, which allow for once-weekly administration in research settings. [nature.com] [link.springer.com]

Current literature positions Tirzepatide as a subject of interest for understanding receptor selectivity, biased signaling, and metabolic pathway integration in incretin biology. Ongoing research continues to evaluate its mechanistic properties and broader implications for metabolic homeostasis. [mdpi.com]

Key Peer-Reviewed References

1. Structural determinants of dual incretin receptor agonism by tirzepatide. PNAS. 2022. DOI:10.1073/pnas.2116506119 [pnas.org]
2. The incretin co-agonist tirzepatide requires GIPR for hormone secretion from human islets. Nature Metabolism. 2023. DOI:10.1038/s42255-023-00811-0 [nature.com]
3. Insights into the Mechanism of Action of Tirzepatide: A Narrative Review. Diabetes Therapy. 2025. Springer [link.springer.com]
4. Novel Dual Incretin Receptor Agonists in the Spectrum of Metabolic Diseases with a Focus on Tirzepatide. Biomedicines. 2023. DOI:10.3390/biomedicines11071875