Product Information
Catalog Number:
DCA1129bBA1
Lot Number:
DCA1129bBA1-020626
Quantity:
1 vial (4 x 106) frozen cells
Freeze Medium: Cellbanker 2
Host cell:
HEK293T β-Arrestin1
Transfection: Expression vector containing full-length human GPR75 cDNA (GenBank accession number AF072693.1) with FLAG tag sequence at N-terminus
Recommended Storage:
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS
Data Sheet
Background: GPR75 is a class A orphan G protein-coupled receptor expressed in most tissues, but highly expressed in the brain. Studies have suggested that GPR75 is involved in hypertension, metabolic syndrome, obesity, and cancer, and may be a viable therapeutic target for the treatment of these conditions. Binding studies have shown that the eicosanoid 20-hydroxyeicosatetraenoic acid (20-HETE) and the chemokine CCL5 (RANTES) bind to GPR75, but the outcomes of these binding interactions are disputed. GPR75 associates with Gαq, and therefore its activation should result in an increase in [cytoplasmic Ca2+] through the phospholipase C / inositol triphosphate pathway.
Application: Functional assays
Figure 1. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP accumulation upon treatment with ligand, measured with MULTISCREENTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01).
References:
Pascale et al. (2021) Uncovering the signalling, structure and function of the 20-HETE-GPR75 pairing: Identifying the chemokine CCL5 as a negative regulator of GPR75. Br J Pharmacol. 178:3813-3828.
Dashti et al. (2023) G Protein-Coupled Receptor 75 (GPR75) As a Novel Molecule for Targeted Therapy of Cancer and Metabolic Syndrome. Asian Pac J Cancer Prev. 24(5):1817-1825.
Ignatov et al. (2006) RANTES stimulates Ca2+ mobilization and inositol triphosphate (IP3) formation in cells transfected with G protein-coupled receptor 75. Br J Phamacol. 149:490-497.
Garcia et al. (2017) 20-HETE Signals Through G Protein-Coupled Receptor GPR75 (Gq) to Affect Vascular Function and Trigger Hypertension. Circ Res. 120(11):1776-1788.