Biochem/physiol Actions

DJ-V-159 is an agonist of GPRC6A, a family C G protein coupled receptor proposed to be master regulator of energy metabolism. GPRC6A is the receptor for osteocalcin, basic amino acids (e.g., L-Arginine), cations (e.g., calcium), and is a membrane receptor for testosterone. DJ-V-159 activated GPRC6A at 0.2 nM concentrations and stimulated GPRC6A-mediated ERK phosphorylation and cAMP accumulation in GPRC6A expressing HEK-293 cells. DJ-V-159 was found to stimulate insulin secretion from mouse β-cells and and lower serum glucose in wild-type mice.