DJ-V-159

DJ-V-159 (CAS No.: 2253744-53-3) is a small-molecule agonist of the G protein-coupled receptor family C group 6 member A (GPRC6A), a receptor implicated in nutrient sensing and metabolic regulation, and is widely utilized as a pharmacological tool in receptor signaling and metabolic research. This compound selectively activates GPRC6A-mediated signaling pathways, including extracellular signal-regulated kinase (ERK) phosphorylation and cyclic AMP (cAMP) production, in engineered cell systems such as GPRC6A-transfected HEK-293 cells, while showing minimal activity in non-transfected controls, indicating receptor-dependent specificity; its functional potency is comparable to endogenous ligands such as L-arginine and is observed at low nanomolar concentrations in vitro. In addition, DJ-V-159 has been shown to stimulate insulin secretion in pancreatic β-cell models, such as MIN-6 cells, supporting its relevance for studying receptor-mediated endocrine responses. In vivo experimental studies in mice demonstrate that systemic administration can modulate glucose levels without overt acute toxicity under controlled conditions, highlighting its utility in probing GPRC6A-related metabolic pathways. The concentrations or doses employed in experimental settings vary depending on assay design and biological context, making DJ-V-159 a valuable reagent for mechanistic studies, target validation, and early-stage drug discovery efforts focused on GPRC6A signaling.