DJ-V-159

Cas No.:	2253744-53-3
Chemical Name:	DJ-V-159
Synonyms:	DJ-V-159
SMILES:	C1(C(NC2=CC(=C(C=C2)C#N)C(F)(F)F)=O)C=C(C=CC=1)C(NC1C=CC(C#N)=C(C(F)(F)F)C=1)=O
Formula:	C24H12F6N4O2
M.Wt:	502.37
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
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].
In Vitro:	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].
Animal Administration:	Mice[1] 8 to 10 weeks ago wild type C57BL/6 mice are fasted for 5 hours, injected ip with ${DJ-V-159} (10 mg/kg body weight), or Metformin (300 mg/kg body weight), or vehicle (95% PEG + 5% DMSO; 10 μL/g body weight). Blood glucose levels are measured at 0, 30, 60 and 90 minutes after injection[1].
References:	[1]. Pi M, et al. Computationally identified novel agonists for GPRC6A. PLoS One. 2018 Apr 23;13(4):e0195980.