| Bioactivity | DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A). | ||||||||||||
| Target | GPRC6A. | ||||||||||||
| Invitro | DJ-V-159 activates ERK in HEK-293 transfected with GPRC6A but not in non-transfected HEK-293 cells, with potency similar to L-Arg. In addition, DJ-V-159 dose-dependently stimulates cAMP production in GPRC6A expressing HEK-293 cells, achieving a response a 0.2 nM concentrations in the media. DJ-V-159 stimulates insulin secretion in mouse beta-cell MIN-6 cells. The DJ-V-159 increased insulin stimulation index (SI) in MIN-6 cells similar to the effects of Ocn, known ligand of GPRC6A[1]. | ||||||||||||
| In Vivo | DJ-V-159 at the dose of 10 mg/kg reduces blood glucose levels in wildtype mice at 60 and 90 minutes after intraperitoneal administration of 10 mg/kg, whereas the vehicle (95% PEG + 5% DMSO) has no effect on blood glucose. DJ-V-159 reduces blood glucose levels in wild-type mice by 43.6% and 41.9% at 60 and 90 minutes, respectively, after intraperitoneal administration of 10 mg/kg. 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]. | ||||||||||||
| Name | DJ-V-159 | ||||||||||||
| CAS | 2253744-53-3 | ||||||||||||
| Formula | C24H12F6N4O2 | ||||||||||||
| Molar Mass | 502.37 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Pi M, et al. Computationally identified novel agonists for GPRC6A. PLoS One. 2018 Apr 23;13(4):e0195980. |