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DJ-V-159 

Cat. No.: HY-114165 Purity: 99.99%
Handling Instructions

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

For research use only. We do not sell to patients.

DJ-V-159 Chemical Structure

DJ-V-159 Chemical Structure

CAS No. : 2253744-53-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 440 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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].

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].

Molecular Weight

502.37

Formula

C₂₄H₁₂F₆N₄O₂

CAS No.

2253744-53-3

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

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
In Vitro: 

DMSO : 25 mg/mL (49.76 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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DJ-V-159
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