HUMAN RECOMBINANT GPR81 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Cell Banker 2 (Amsbio 11891)
Full-length Human GPR81 (GenBank Accession Number NM_032554.3) with FLAG-tag sequence at the N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Stable in culture for minimum of two months
Background: GPR81 is an orphan G protein-coupled receptor homologous to GPR109A and GPR109B. It is highly expressed in adipose tissues and also regarded as a sensor for Lactate and can mediate an anti-lipolytic effect of lactate. GPR81 can modulate the free fatty acid pool under exercise or conditions of oxygen deficit and is target for the treatment of dyslipidemia and other metabolic disorders.
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). 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.
Ge et al (2008) Elucidation of signaling and functional activities of an orphan GPCR, GPR81. Journal of Lipid Research 49:797-803.
Liu et al. (2009) Lactate Inhibits Lipolysis in Fat Cells through Activation of an Orphan G-protein-coupled Receptor, GPR81. Journal of Biological Chemistry 284: 2811–2822.
Cai et al (2008) Role of GPR81 in lactate-mediated reduction of adipose lipolysis. Biochem Biophys Res Commun, 377(3): 987-991