Human MC4R Stable Cell Line - HEK293

The melanocortin 4 receptor (MC4R) is an important G protein-coupled receptor primarily expressed in the central nervous system, particularly in the hypothalamus, a region regulating energy homeostasis. As a key participant in the melanocortin pathway, MC4R is activated by α-melanocyte-stimulating hormone (α-MSH) and inhibited by hamster-related peptide (AgRP). This receptor is a crucial regulator of appetite suppression, energy expenditure, and weight control. Mutations in the MC4R gene are the most common monogenic cause of severe early-onset obesity in humans. Dysregulation of MC4R signaling leads to overeating, reduced energy expenditure, and insulin resistance, making it a major therapeutic target for obesity and related metabolic disorders. The complex signaling mechanisms of this receptor—including regulation of adenylate cyclase activity and cAMP production—underlie its important physiological role in energy balance and autonomic nervous function.

The human MC4R stable cell line HEK293 is a genetically engineered cell model specifically designed for high-throughput screening and functional characterization of MC4R-targeting compounds. This cell line was constructed by stably transfecting the human MC4R gene into human embryonic kidney cells (HEK293), enabling stable and efficient receptor expression while maintaining cell viability and function. HEK293 cells, with their high transfection efficiency, rapid growth, and ability to undergo post-translational modifications, are ideal host cells, ensuring proper receptor transport and membrane localization. This cell line allows researchers to study MC4R ligand binding affinity, receptor activation kinetics, downstream signaling pathways (e.g., cAMP accumulation assays), and receptor desensitization mechanisms. Its stability eliminates experimental errors introduced by transient transfection, making it invaluable in drug development projects targeting obesity, metabolic syndrome, and cachexia. Applications include screening MC4R agonists/antagonists, studying the functional consequences of receptor mutations, and validating the efficacy and specificity of therapeutic candidates.