PathHunter® Human ADCYAP1R1 (PAC1) Total GPCR Internalization Cell-Based Assay Kit (U2OS)

Background Information:

The PathHunter® Human ADCYAP1R1 (PAC1) Total GPCR Internalization Cell-Based Assay Kit (U2OS) utilizes the ADCYAP1R1 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., PACAP) based internalization of ADCYAP1R1 via detection of localization to the early endosome. This product uses EFC technology. The included cell line overexpresses PK-tagged ADCYAP1R1 and an EA-tagged early endosome protein. Upon ligand-induced receptor activation, the internalization of the ADCYAP1R1 receptor to the early endosome results in the 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:

VIP and PACAP

Sub Family:

Class B

Coupling:

Gq & Gs

Protein Name:

PAC1 (PACAP)

Protein Aliases:

PACAP-R-1|PACAP-R1|PACAP receptor 1

Accession Number:

AY366498; NM_001118

UniProt Number:

P41586

Gene Name:

ADCYAP1R1

Gene ID:

117

Gene Aliases:

PAC1|PACAPR|PAC1R

Target Species:

Human

Cell Background:

U2OS