DJ-V-159

• CAT Number: I019665
• CAS Number: 2253744-53-3
• Molecular Formula: C24H12F6N4O2
• Molecular Weight: 502.37
• Purity: ≥95%
• Synonyms: 1-N,3-N-bis[4-cyano-3-(trifluoromethyl)phenyl]benzene-1,3-dicarboxamide
• InChI: InChI=1S/C24H12F6N4O2/c25-23(26,27)19-9-17(6-4-15(19)11-31)33-21(35)13-2-1-3-14(8-13)22(36)34-18-7-5-16(12-32)20(10-18)24(28,29)30/h1-10H,(H,33,35)(H,34,36)
• InChIKey: VEVNLJLJLVESLL-UHFFFAOYSA-N
• SMILES: C1=CC(=CC(=C1)C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)C(=O)NC3=CC(=C(C=C3)C#N)C(F)(F)F

DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
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].
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].

Reference

[1]. Pi M, et al. Computationally identified novel agonists for GPRC6A. PLoS One. 2018 Apr 23;13(4):e0195980.
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