PathHunter® eXpress PTHR1 Activated GPCR Internalization Assay

Background Information:

The PathHunter® PTHR1 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. PTH) based internalization of PTHR1 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 PTHR1. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting PTHR1-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:

Parathyroid Hormone

Sub Family:

Class B

Coupling:

Gq & Gs

Protein Name:

PTH1

Protein Aliases:

PTH/PTHr receptor|Parathyroid hormone 1 receptor|PTH1 receptor

Accession Number:

AY449732

UniProt Number:

Q03431

Gene Name:

PTH1R

Gene ID:

5745

Target Species:

Human

Cell Background:

U2OS