Tirzepatide (LY3298176) is a novel, 39-amino-acid linear synthetic peptide designed to function as a “twincretin,” or dual GIP and GLP-1 receptor agonist. By simultaneously targeting both of these key incretin hormone receptors, it mimics their natural effects, leading to a synergistic enhancement of metabolic regulation.

In a research context, its mechanism of action is of significant interest. Activation of the GLP-1 and GIP receptors is known to stimulate first- and second-phase insulin secretion and reduce glucagon levels, both in a glucose-dependent manner. Furthermore, Tirzepatide has been shown to delay gastric emptying, lower food intake, and increase insulin sensitivity.

This dual-agonist approach has made Tirzepatide a subject of extensive clinical investigation for its profound effects on both improving glycemic control in type 2 diabetes and producing substantial weight loss in individuals with obesity or who are overweight.

CAS Number: 2023788-19-2