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VU6005649

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Catalog No. T13321Cas No. 2137047-43-7

VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).

VU6005649

VU6005649

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Purity: 99.87%
Catalog No. T13321Cas No. 2137047-43-7
VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$37In StockIn Stock
25 mg$75In StockIn Stock
50 mg$121In StockIn Stock
100 mg$191In StockIn Stock
200 mg$272In StockIn Stock
1 mL x 10 mM (in DMSO)$30In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.87%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).
Targets&IC50
mGluR7:0.65 μM (EC50), mGluR8:2.6 μM
In vitro
VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor(EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively). VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50.
In vivo
In wild-type mice VU6005649 shows modest but significant pro-cognitive effects on associative learning and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model.
Chemical Properties
Molecular Weight357.28
FormulaC16H12F5N3O
Cas No.2137047-43-7
SmilesCOc1ccc(-c2c(C)nn3c(cc(C)nc23)C(F)(F)F)c(F)c1F
Relative Density.1.43 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 60 mg/mL (167.94 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.6 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7989 mL13.9946 mL27.9893 mL139.9463 mL
5 mM0.5598 mL2.7989 mL5.5979 mL27.9893 mL
10 mM0.2799 mL1.3995 mL2.7989 mL13.9946 mL
20 mM0.1399 mL0.6997 mL1.3995 mL6.9973 mL
50 mM0.0560 mL0.2799 mL0.5598 mL2.7989 mL
100 mM0.0280 mL0.1399 mL0.2799 mL1.3995 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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