Product Information
Catalog Number:
C1117
Lot Number:
C1117-012725
Quantity:
1 vial (2 x 106) frozen cells
Freeze Medium:
Cellbanker 2
Host cell:
HEK293T
Transfection:
Full-length human GPR61 cDNA (GenBank Accession Number NM_031936.3) with FLAG tag sequence at N-terminus
Recommended Storage:
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 µg/mL puromycin
Stability:
In progress
Data Sheet
Background: G-protein-coupled receptor 61 (GPR61) is a receptor for a tertiary sulfonamide. It is expressed in the hypothalamus and brainstem. While not fully understood, studies suggest that GPR61 could be linked to conditions such as type 2 diabetes. Because of this, GPR61 is a possible target for appetite modulation. In concert with several other GPCRs, GPR61 is also responsible for plasmalogen mediation, which is necessary for neuronal cell survival. Additionally, GPR61 co-colonizes with Gonadotropin-releasing hormone receptors on gonadotrophs, which play a vital role in reproductive function.
Application: Functional assays
Figure 1. Dose-dependent increase of intracellular cAMP accumulation upon treatment with ligand, measured with MULTISCREEN™ TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 2. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
References:
Lees, et al. (2023) An inverse agonist of orphan receptor GPR61 acts by a G protein competitive allosteric mechanism. Nat. Commun 14:5938.
Hossian, et al. (2016) Neuronal Orphan G-Protein Coupled Receptor Proteins Mediate Plasmalogens-Induced Activation of ERK and Akt Signaling. PLOS ONE DOI:10.1371/journal.pone.0150846.
Kadokawa, et al. (2022) Chemosynthetic ethanolamine plasmalogen stimulates gonadotropin secretion from bovine gonadotrophs by acting as a potential GPR61 agonist. Anim. Reprod. Sci. 241:106992.
Kozielewicz, et al. (2019) Overexpression of Orphan Receptor GPR61 Increases cAMP Levels upon Forskolin Stimulation in HEK293 Cells: in vitro and in silico Validation of 5-(Nonyloxy) Tryptamine as a Low-Affinity Inverse Agonist. Pharmacology 104:377–382.