PathHunter® eXpress AGTRL1 Activated GPCR Internalization Assay

Background Information:

The PathHunter® AGTRL1 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. apelin-13) based internalization of AGTRL1 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 AGTRL1. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting AGTRL1-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:

Apelin

Sub Family:

Class A

Coupling:

Gi/Go

Protein Name:

APJ

Protein Aliases:

APJ (apelin) receptor

Accession Number:

NM_005161

UniProt Number:

P35414

Gene Name:

APLNR

Gene ID:

187

Gene Aliases:

FLJ90771|APJ|APJR

Target Species:

Human

Cell Background:

U2OS