PathHunter® Human CHRM5 Stable Cell Line Activated GPCR Internalization Assay (U2OS)

Background Information:

The PathHunter Human CHRM5 Stable Cell Line Activated GPCR Internalization Assay (U2OS) utilizes the CHRM5 Activated GPCR Internalization cell line. The stable engineered cell line is designed for use in studying drug candidates (small molecules or biologics) that affect GPCR activation and internalization. This cell line enables the assessment of ligand (e.g., acetylcholine)- based internalization of CHRM5 via the detection of localization to the early endosome. This product uses EFC technology. The included cell line overexpresses EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged CHRM5. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CHRM5-arrestin complex is internalized to the early endosome, leading to production of EFC signal.
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. Assay plates and positive control for use in the assays can be purchased separately. For continued use of the cell line, additional quantities of cell culture and assay reagents are available for purchase separately.
Eurofins DiscoverX optimized Detection Reagents are required for optimal assay performance and must be used with these cell lines in accordance with the cell line license agreed to upon purchase of this cell line assay kit.

Target Class:

GPCR

Family:

Acetylcholine (Muscarinic)

Sub Family:

Class A

Coupling:

Gq

Protein Name:

M5

Protein Aliases:

acetylcholine receptor, muscarinic 5

Accession Number:

AF498919

UniProt Number:

P08912

Gene Name:

CHRM5

Gene ID:

1133

Target Species:

Human

Cell Background:

U2OS