DJ-V-159 is a GPRC6A agonist, targeting the G protein-coupled receptor family C group 6 member A (GPRC6A).

DJ-V159 activates ERK in HEK-293 cells transfected with GPRC6A but not in non-transfected HEK-293 cells, with potency similar to L-Arg. Additionally, DJ-V159 dose-dependently stimulates cAMP production in GPRC6A-expressing HEK-293 cells at 0.2 nM concentrations in the media. DJ-V159 also stimulates insulin secretion in mouse beta-cell MIN-6 cells, with an insulin stimulation index (SI) similar to Ocn, a known ligand of GPRC6A [1].

DJ-V-159 (10 mg/kg, i.p.) reduces blood glucose levels in wild-type mice at 60 and 90 minutes, whereas the vehicle (95% PEG + 5% DMSO) has no effect on blood glucose. DJ-V-159 (10 mg/kg, i.p.) reduces blood glucose levels in wild-type mice by 43.6% and 41.9% at 60 and 90 minutes, respectively. The mice tolerated this short-term exposure to DJ-V-159 without any overt side-effects. DJ-V-159, however, is almost in or on the boundary of the Lipinski's Rule of Five [1].