PathHunter® eXpress VIPR1 Activated GPCR Internalization Assay

Background Information:

The PathHunter® VIPR1 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. VIP) based internalization of VIPR1 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 VIPR1. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting VIPR1-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:

VIP and PACAP

Sub Family:

Class B

Coupling:

Gq & Gs

Protein Name:

VIP1 (VPAC1)

Protein Aliases:

PVR2|HVR1|RDC1|VIP and PACAP receptor 1|PACAP-R2|pituitary adenylate cyclase-activating polypeptide type II receptor|VIP-R1

Accession Number:

NM_004624

UniProt Number:

P32241

Gene Name:

VIPR1

Gene ID:

7433

Gene Aliases:

VPAC1|RDC1|HVR1|VPAC1R

Target Species:

Human

Cell Background:

U2OS