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:

KitComponent

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®