Product Description

The gastric inhibitory polypeptide receptor (GIPR) is a class B G protein-coupled receptor that specifically binds glucose-dependent insulinotropic polypeptide (GIP). It is primarily distributed in pancreatic β-cells, adipocytes, bone cells, and the central nervous system. Its core function is to mediate the diverse physiological actions of GIP: in the pancreas, it stimulates glucose-dependent insulin secretion postprandially; in adipose tissue, it enhances lipid synthesis and storage; and in bone, it regulates bone formation and turnover. Thus, GIPR is a key receptor linking nutrient intake to energy storage. However, in type 2 diabetes, its insulinotropic effect is often blunted while its lipogenic action persists, making it a crucial target for novel “dual (GIPR/GLP-1R) agonists” that synergistically improve both blood glucose and body weight.

ScreeningBio’s Rat GIPR β-arrestin cell line is an ideal tool for studying GPCR/β-arrestin interactions. In this system, the GPCR C-terminus is fused to a smallBiT tag, and the β2-arrestin N-terminus is fused to a largeBiT tag. Upon receptor activation, GPCR/β-arrestin interaction brings the two fragments together to reconstitute an active NanoLuc enzyme, which can be quantified using the NanoBiT substrate. This cell line is designed to evaluate a compound’s ability to activate the β-arrestin signaling pathway.