Biological Information
Background Information:
The PathHunter® Human GLP-1 (GLP-1 Receptor) Total GPCR Internalization Cell-Based Assay Kit (U2OS) utilizes the GLP1R Total GPCR internalization cell line. The stable engineered cell line is for use in studying drug candidates (small molecules or biologics) affecting GPCR activation and internalization. This cell line enables assessment of ligand (e.g. exendin-4) based internalization of GLP1R via detection of localization to the early endosome. This product uses EFC technology. The included cell line overexpresses PK-tagged GLP1R and an EA-tagged early endosome protein. Upon ligand-induced receptor activation, the resulting internalization of the GLP1R receptor to the early endosome leads to production of the EFC signal. This product leverages a sensitive chemiluminescent detection system that delivers a wide dynamic range and robust Z’ for potency, efficacy, and rank‑order profiling across small molecules and biologics.
This kit includes a stable engineered cell line (supplied as two vials of cryopreserved cells); cell line specific reagents for cell thawing, propagation, detachment, cryopreservation, and cell plating; and a 10‑plate detection kit required to run the assay.
All additional cell culture and assay reagents are available for purchase separately.
Target Class:
GPCR
Family:
Glucagon
Sub Family:
Class B
Coupling:
Gs
Protein Name:
GLP-1
Protein Aliases:
GLP-1-R|GLP-1R
Accession Number:
NM_002062.3
UniProt Number:
P43220
Gene Name:
GLP1R
Gene ID:
2740
Target Species:
Human
Cell Background:
U2OS
Usage
Product Type:
Cell Line Assay Kits
Application:
Drug Discovery & Development
Kit Components:

Storage Conditions:
Store in vapor phase of liquid nitrogen.
Usage disclaimer:
These products may be covered by issued US and/or foreign patents, patent applications and subject to a Limited Use Label License. Please visit discoverx.com/license for a list of products that are governed by limited use label license terms and relevant patent and trademark information.
Assay Information
Assay Type:
Cell Based
Assay Measures:
Internalization
Detection Method:
Chemiluminescence
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
PathHunter®