[CAS NO. 2253744-53-3] DJ-V-159
PRODUCTS SPECIFICATIONS [2253744-53-3]
DESCRIPTION [2253744-53-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 502.37 |
| Molecular Formula | C24H12F6N4O2 |
| SMILES | O=C(C1=CC(C(NC2=CC(C(F)(F)F)=C(C#N)C=C2)=O)=CC=C1)NC3=CC(C(F)(F)F)=C(C#N)C=C3 |
Summary
DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A) .
IC50 & Target
GPRC6A [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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 49.76 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9906 mL | 9.9528 mL | 19.9056 mL |
| 5 mM | 0.3981 mL | 1.9906 mL | 3.9811 mL |
| 10 mM | 0.1991 mL | 0.9953 mL | 1.9906 mL |
