Human GPR146 Stable Cell Line - HEK293

GPR146 (G protein-coupled receptor 146), also known as PGR8, is an orphan class A GPCR encoded by the gene located on chromosome 7p22.3. The receptor is expressed in a broad range of human tissues including adipose tissue, lung, and liver, and has been shown to couple to Gi/o proteins, leading to inhibition of adenylate cyclase and reduction of intracellular cAMP levels. Recent genome-wide association studies have linked GPR146 to plasma lipid regulation, and loss-of-function studies in both mice and humans suggest that GPR146 plays a significant role in cholesterol homeostasis, making it an emerging therapeutic target for hypercholesterolemia and atherosclerosis. The Human GPR146 Stable Cell Line - HEK293 is generated by transfecting the full-length human GPR146 coding sequence into HEK293 host cells, followed by antibiotic selection and clonal isolation to establish a population that stably and constitutively expresses the receptor on the plasma membrane. This cell line provides a reliable and reproducible cell-based platform designed for functional studies of GPR146 without the need for repeated transient transfections.

This stable cell line supports a variety of applications in GPCR research and drug discovery. It is particularly suited for cell-based assays such as cAMP modulation measurements, which can be used to evaluate the Gi/o coupling activity of GPR146 in response to candidate ligands or test compounds. Researchers can also employ this line in beta-arrestin recruitment assays, internalization studies, and calcium flux measurements when combined with chimeric G proteins. Because GPR146 remains an orphan receptor with no fully validated endogenous ligand, this cell line offers a valuable tool for deorphanization efforts and for screening small-molecule libraries aimed at identifying agonists or inverse agonists. Additionally, the line can be used to study downstream signaling pathways involving ERK phosphorylation and to investigate the receptor’s role in cholesterol metabolism through co-culture or gene expression analysis.