CHO-K1 Human GLP-1R β Arrestin Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-A-0106A | Inquiry |
Compound Testing Services | CT-001 | $1,850 per 384w plate (Up To 16 cpds Dose) |
Product Description
The Glucagon-Like Peptide-1 Receptor (GLP-1R) is a class B G protein-coupled receptor (GPCR) that plays a central role in glucose metabolism by mediating the effects of the incretin hormone GLP-1. GLP-1R is primarily expressed in pancreatic β-cells, as well as in the gastrointestinal tract and central nervous system. Activation of GLP-1R enhances glucose-dependent insulin secretion, inhibits glucagon release, delays gastric emptying, and promotes satiety.
ScreeningBio’s human GLP-1R 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.
Product Specifications
Target Type | GPCR |
Species | Human |
HGNC Symbol | GLP-1R |
Accession Number | NM_002062 |
Parental Line | HEK293 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
Target Background
The glucagon-like peptide-1 receptor (GLP-1R) is a class B G-protein-coupled receptor (GPCR) that plays a central role in glucose homeostasis and energy balance. GLP-1R is primarily expressed in pancreatic β-cells, but is also found in the central nervous system, gastrointestinal tract, cardiovascular system, and kidney. Its broad tissue distribution underlies both metabolic and extra-metabolic effects.
Upon binding to its endogenous agonist GLP-1, secreted postprandially from intestinal L-cells, GLP-1R undergoes a conformational change that activates Gs proteins. This leads to stimulation of adenylate cyclase, elevation of intracellular cAMP, and downstream activation of protein kinase A (PKA) and Epac signaling pathways. In pancreatic β-cells, this signaling enhances glucose-dependent insulin secretion, suppresses glucagon release, and promotes cell survival. In the CNS, GLP-1R activation contributes to satiety, reduced food intake, and weight control, while in the cardiovascular system it has been linked to cardioprotective effects.
GLP-1R is an established therapeutic target for type 2 diabetes mellitus and obesity. GLP-1R agonists (e.g., exenatide, liraglutide, semaglutide) are widely used to improve glycemic control and induce weight loss, with additional benefits on cardiovascular outcomes. Small-molecule agonists and positive allosteric modulators are also under investigation to expand therapeutic options. Conversely, receptor antagonists such as exendin(9-39) have been used in experimental settings to probe physiological function. Because of its multifaceted role in metabolic regulation and cardiovascular health, GLP-1R continues to be a major focus in both drug discovery and translational research.