Tirzepatide Peptide

Tirzepatide is a synthetic dual receptor agonist peptide designed for investigation of metabolic and endocrine signaling pathways. Structurally, it is a linear 39-amino acid synthetic peptide conjugated to a C20 fatty diacid moiety via a hydrophilic linker. This design enhances its stability and extends its half-life, making it a unique compound in research on incretin hormone activity.

Tirzepatide is engineered to act as a dual agonist of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. These receptors are integral to the regulation of glucose metabolism, energy balance, and appetite. In laboratory models, Tirzepatide has demonstrated the ability to activate signaling cascades associated with both incretins, potentially offering a synergistic effect on insulin secretion, glucagon suppression, and central appetite regulation.

Chemical Makeup

• Molecular Formula: C225H348N48O68

• Molecular Weight: 4813.52 g/mol

• Sequence (Simplified): Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Gly-Ala-Ile-Ala-Gln-Lys-Asn-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly

• Modifications: C20 fatty diacid side chain for albumin binding and metabolic resistance

Research & Preclinical Investigations

Tirzepatide as a Dual Incretin Receptor Agonist

In vivo studies using non-human primate and murine models have shown that Tirzepatide can simultaneously activate GIP and GLP-1 pathways. This dual action may enhance insulinotropic effects under hyperglycemic conditions, reduce hepatic glucose output, and promote satiety through hypothalamic signaling.

Tirzepatide and Metabolic Regulation

Rodent models exposed to Tirzepatide have demonstrated reductions in body weight, fat mass, and food intake. These effects are hypothesized to be due to delayed gastric emptying and modulation of central reward-related appetite pathways. Additionally, studies have shown a significant reduction in circulating lipids and improved insulin sensitivity markers.

Pharmacokinetics of Tirzepatide

Tirzepatide’s fatty acid modification facilitates albumin binding, leading to extended systemic exposure. In experimental subjects, the reported half-life has ranged from 4 to 5 days, supporting once-weekly administration in dose-dependent research protocols.

Research Use Only

Tirzepatide is offered strictly for in vitro and in vivo non-clinical research use. It is not intended for human or veterinary use, diagnostic procedures, or therapeutic applications. All laboratory handling must conform to institutional biosafety and regulatory guidelines.

References

1. Frias JP, Nauck MA, Van J, et al. Efficacy and safety of Tirzepatide, a dual GIP and GLP-1 receptor agonist: a randomized, double-blind, placebo-controlled study in type 2 diabetes. Lancet. 2021;398(10295):143-155.

2. Coskun T, Sloop KW, Loghin C, et al. Tirzepatide, a novel dual GIP/GLP-1 receptor agonist for the treatment of type 2 diabetes: Mechanistic basis and preclinical profile. Cell Metab. 2018;27(4):740-756.e9.

3. Drucker DJ. Mechanisms of action and therapeutic application of GLP-1 and GIP receptor agonists in metabolic disease. Nat Rev Endocrinol. 2022;18(4):214–234.

4. Min T, Bain SC. The role of Tirzepatide, dual GIP and GLP-1 receptor agonist, in the management of type 2 diabetes: A review. Diabetes Ther. 2021;12(1):143–157.