Human MC3R Stable Cell Line - HEK293

The melanocortin-3 receptor (MC3R) is a class A G protein-coupled receptor (GPCR) encoded by the MC3R gene located on human chromosome 20. It is one of five melanocortin receptors that respond to peptides derived from promelanocyte-stimulating hormone (POMC), including α-MSH, β-MSH, γ-MSH, and ACTH, with spiky-associated peptide (AgRP) acting as an endogenous antagonist/reverse agonist. MC3R is primarily coupled to Gs proteins, stimulating adenylate cyclase and increasing intracellular cAMP levels; however, the cellular environment influences the complexity of signal transduction, including activation of other pathways and β-arrestin-dependent processes. Physiologically, MC3R is expressed in the hypothalamus and limbic system regions, participating in energy homeostasis, nutrient allocation, and the coordination of feeding behavior with circadian rhythms and metabolic signaling. Genetic studies have shown that MC3R variations are associated with altered fat deposition, growth, and metabolic flexibility, exhibiting a phenotype distinct from MC4R. In addition to its metabolic effects, MC3R has been reported to influence inflammatory and immune responses, reflecting the broader role of melanocortin in peripheral tissues.

The human MC3R stable cell line HEK293 is a research-grade cell model that is genetically engineered to constitutively express human MC3R in a well-defined HEK293 cell line. The low background of endogenous melanocortin receptors in HEK293 host cells facilitates the clear detection of MC3R-specific pharmacological properties. This cell line is compatible with various GPCR assays, including cAMP accumulation assays, CRE-driven reporter gene assays, β-arrestin recruitment assays, and equilibrium or kinetic ligand binding assays, enabling comprehensive analysis of agonists, partial agonists, antagonists, inverse agonists, and allosteric modulators. It is well-suited for high-throughput screening and structure-activity relationship studies, potency and efficacy ranking, signal bias assessment, and selectivity comparisons with other melanocortin receptors.