HUMAN RECOMBINANT MC4 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human MC4R cDNA (GenBank Accession Number NM_005912.2) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Stable for a minimum of two months in culture
Background: The melanocortin receptor MC4 is expressed in the central nervous system, gastrointestinal tract and placenta. The melanocortin family is essential in the control of body weight homeostasis, sexual behavior, and autonomic functions; MC4 receptors are primarily involved in the regulation of food uptake. MC4 agonists have great potential in the treatment of weight disorders and sexual dysfunction, whereas MC4 antagonists may be useful in the treatment of anorectic and cachectic conditions.
Application: Functional assays
Figure 1. Dose-dependent stimulation of intracellular cAMP level upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 2. Dose-dependent stimulation of calcium flux upon treatment with ligand, monitored with FlexStation. Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Gantz et al. (1993) Molecular cloning of a novel melanocortin receptor. J Biol Chem 268:8246-8250.
Voisey et al. (2003) Melanocortins and their receptors and antagonists. Curr Drug Targets 4:589-597.
Wikberg et al. (2008) Targeting melanocortin receptors: an approach to treat weight disorders and sexual disorders. Nat Rev Drug Discov 7:307-323.