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VU0650786

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Catalog No. T13318Cas No. 1809085-30-0

VU0650786 is a selective and potent CNS-penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), exhibiting antidepressant and anxiolytic activity in rodents.

VU0650786

VU0650786

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Purity: 99.09%
Catalog No. T13318Cas No. 1809085-30-0
VU0650786 is a selective and potent CNS-penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), exhibiting antidepressant and anxiolytic activity in rodents.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$97In StockIn Stock
5 mg$247In StockIn Stock
10 mg$347In StockIn Stock
25 mg$589In StockIn Stock
50 mg$842In StockIn Stock
100 mg$1,160-In Stock
1 mL x 10 mM (in DMSO)$272In 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:99.09%
Appearance:Solid
Color:White
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Product Introduction

VU0650786 AI Summary
VU0650786 exhibits negative allosteric modulation of both rat mGlu3 and mGlu5 receptors, with IC50 values of 389.05 nM and 392.0 nM, respectively. It also displays calcium mobilization activity in these assays. The compound has shown binding affinity to the 5HT2B receptor, selectivity ratios, and the ability to inhibit certain enzymes in human liver microsomes. Additionally, it demonstrates specific plasma concentration, drug uptake, and distribution characteristics in rat and mouse models. In terms of antiviral activity, VU0650786 shows 7.34% inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM. However, it demonstrates 0.0% inhibition of SARS-CoV-2 induced cytotoxicity in VERO-6 cells at a concentration of 10 µM after 48 hours of exposure..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
VU0650786 is a selective and potent CNS-penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), exhibiting antidepressant and anxiolytic activity in rodents.
Targets&IC50
mGluR3:392 nM
Chemical Properties
Molecular Weight387.8
FormulaC18H15ClFN5O2
Cas No.1809085-30-0
SmilesC[C@@H]1CN(C(=O)c2cc(COc3ccc(Cl)cn3)nn12)c1cccnc1F
Relative Density.1.49 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
H2O: insoluble
DMSO: 240 mg/mL (618.88 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (12.89 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 mM2.5786 mL12.8932 mL25.7865 mL128.9324 mL
5 mM0.5157 mL2.5786 mL5.1573 mL25.7865 mL
10 mM0.2579 mL1.2893 mL2.5786 mL12.8932 mL
20 mM0.1289 mL0.6447 mL1.2893 mL6.4466 mL
50 mM0.0516 mL0.2579 mL0.5157 mL2.5786 mL
100 mM0.0258 mL0.1289 mL0.2579 mL1.2893 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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Tech Support

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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