PathHunter® eXpress F2RL1 Activated GPCR Internalization Assay

Background Information:

The PathHunter® F2RL1 Activated GPCR internalization eXpress kit provides an easy to-use cell based assay to study drug candidates affecting GPCR activation and internalization. This kit assesses ligand (e.g. serine proteases, SLIGRL) based internalization of F2RL1 via detection of localization to the early endosome. This product uses EFC technology. The cells included overexpress EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged F2RL1. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting F2RL1-arrestin complex is internalized to the early endosome, leading to production of EFC signal. eXpress kits are a convenient, ready-to-use format which contains all materials needed to run the assay, including single-use vials of cryopreserved cells, cell plating media, detection reagent, and assay plates.

Target Class:

GPCR

Family:

Proteinase-Activated

Sub Family:

Class A

Coupling:

Gi/Go & Gq

Protein Name:

PAR2

Protein Aliases:

proteinase-activated receptor-2

Accession Number:

NM_005242.4

UniProt Number:

P55085

Gene Name:

F2RL1

Gene ID:

2150

Gene Aliases:

PAR2|GPR11

Target Species:

Human

Cell Background:

U2OS