1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. VU6012962

VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.

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

VU6012962 Chemical Structure

VU6012962 Chemical Structure

CAS No. : 2313526-86-0

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
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10 mg USD 160 In-stock
50 mg USD 550 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM[1].

IC50 & Target[1]

mGlu7

347 nM (IC50)

In Vitro

VU6012962 is highly selective for mGlu7 versus the other seven mGlu receptor subtypes[1].

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

In Vivo

VU6012962 (1-10 mg/kg; i.p. injection; 60 minutes prior to testing) decreases anxiety in the elevated zero maze (EZM) assay in mice[1].

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

Animal Model: C57Bl/6J male mice (8 weeks old)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: I.p. injections; 60 minutes prior to testing
Result: Increased total time spent in the open arms at a dose of 3 mg/kg. 10 mg/kg did cause a decrease in overall locomotion.
Molecular Weight

448.40

Formula

C21H19F3N4O4

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=C(OCC2CC2)C(OC)=C1)NC3=C(N4C=NC=N4)C=CC(OC(F)(F)F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (278.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2302 mL 11.1508 mL 22.3015 mL
5 mM 0.4460 mL 2.2302 mL 4.4603 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2302 mL 11.1508 mL 22.3015 mL 55.7538 mL
5 mM 0.4460 mL 2.2302 mL 4.4603 mL 11.1508 mL
10 mM 0.2230 mL 1.1151 mL 2.2302 mL 5.5754 mL
15 mM 0.1487 mL 0.7434 mL 1.4868 mL 3.7169 mL
20 mM 0.1115 mL 0.5575 mL 1.1151 mL 2.7877 mL
25 mM 0.0892 mL 0.4460 mL 0.8921 mL 2.2302 mL
30 mM 0.0743 mL 0.3717 mL 0.7434 mL 1.8585 mL
40 mM 0.0558 mL 0.2788 mL 0.5575 mL 1.3938 mL
50 mM 0.0446 mL 0.2230 mL 0.4460 mL 1.1151 mL
60 mM 0.0372 mL 0.1858 mL 0.3717 mL 0.9292 mL
80 mM 0.0279 mL 0.1394 mL 0.2788 mL 0.6969 mL
100 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5575 mL
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VU6012962 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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VU6012962
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HY-114403
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