GeneBLAzer™ MC4R-CRE-bla CHO-K1 cells contain the human Melanocortin Receptor 4 (MC4R) stably integrated into the CellSensor™ CRE-bla CHO-K1 cell line. CellSensor™ CRE-bla CHO-K1 cells (Cat. no. K1535) contain a beta-lactamase reporter gene under control of the Cyclic AMP Response Element (CRE) response element.

The GeneBLAzer™ MC4R-CRE-bla CHO-K1 cells are functionally validated for Z' and EC₅₀ concentrations of α MSH In addition, GeneBLAzer™ MC4R-CRE-bla CHO-K1 cells have been tested for assay performance under variable conditions. These data are found in the Validation & Assay Performance Summary.

MC4 receptors are expressed almost exclusively in the CNS and bind all of the melanocortin peptides, but only have high affinity for α-MSH and ACTH. The agouti peptide binds to the MC4R receptor with high affinity in in vitro tests but, being normally expressed only in skin, doesn't have access to the MC4R receptor under physiological conditions. The AGRP peptide is a high-affinity antagonist of the neural MC4R receptor. The MC4R receptor is involved in the regulation of energy homeostasis and erectile function.

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