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VU6033685

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Catalog No. T205368

VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.

VU6033685

VU6033685

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Catalog No. T205368
VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.
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Product Introduction

Bioactivity
Description
VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.
Chemical Properties
Molecular Weight366.84
FormulaC20H19ClN4O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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

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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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