[Pro3]-GIP (Rat)

Product Name:[Pro3]-GIP (Rat)

Purity:95%

Molar Mass:4970.63

Chemical Formula:C226H343N61O64S

Storage:Store at -20 degrees Celsius

Sequence:YAPGTFISDYSIAMDKIRQQDFVNWLLAQKGKKNDWKHNLTQ

Application:

[Pro3]-GIP (Rat) is a modified analog of the glucose-dependent insulinotropic polypeptide (GIP), a hormone involved in stimulating insulin secretion in response to food intake. In this analog, proline is substituted at the third position, rendering it an antagonist of the GIP receptor. By inhibiting GIP receptor signaling, [Pro3]-GIP is useful in research focused on glucose metabolism, insulin regulation, and type 2 diabetes. It helps explore the role of GIP in metabolic disorders and its potential as a target for therapies aimed at managing conditions like obesity, insulin resistance, and impaired glucose tolerance.

Current Research:

[Pro³]-GIP (Rat) is a synthetic analog of gastric inhibitory polypeptide (GIP), a critical hormone in glucose metabolism and insulin secretion. In this analog, the alanine at position 3 of the peptide sequence is substituted with proline, transforming GIP from a receptor agonist to an antagonist. This structural modification allows [Pro³]-GIP to bind competitively to GIP receptors (GIPR) without activating them, effectively blocking the physiological actions of endogenous GIP.

Mechanism of Action
By inhibiting GIP receptor activation, [Pro³]-GIP reduces the potentiation of glucose-stimulated insulin secretion, a hallmark effect of native GIP. This antagonism provides a tool to investigate the physiological and pathological roles of GIP, particularly in the context of its effects on pancreatic beta-cells, lipid metabolism, and overall glucose homeostasis. The peptide’s antagonistic action also helps explore GIP's influence on energy balance and its implications in obesity and type 2 diabetes.

Research Applications
[Pro³]-GIP is widely used in metabolic research to:

Assess GIP Function: Elucidate GIP's role in glucose regulation and insulin secretion.
Model Disease States: Investigate the contribution of GIP signaling to metabolic disorders, such as obesity and diabetes.
Therapeutic Development: Serve as a prototype for designing GIP receptor antagonists as potential treatments for metabolic diseases.
Conclusion
As a selective GIP receptor antagonist, [Pro³]-GIP offers significant value in studying the complex roles of GIP in metabolic physiology and pathophysiology. By blocking GIP signaling, this peptide aids in advancing our understanding of glucose and energy homeostasis and contributes to the development of therapeutic strategies for managing metabolic disorders. Its application continues to provide critical insights into the potential of targeting GIP pathways for disease intervention.

Reference:

Sparre‐Ulrich, A. H., Hansen, L. S., Svendsen, B., Christensen, M., Knop, F. K., Hartmann, B., … & Rosenkilde, M. M. (2016). Species‐specific action of (Pro3) GIP–A full agonist at human GIP receptors, but a partial agonist and competitive antagonist at rat and mouse GIP receptors. British journal of pharmacology, 173(1), 27-38.