1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. VU0422288

VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice.

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VU0422288 Chemical Structure

VU0422288 Chemical Structure

CAS No. : 1630936-95-6

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Based on 1 publication(s) in Google Scholar

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Description

VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice[1][2].

IC50 & Target

mGluR4

108 nM (EC50)

mGluR7

146 nM (EC50)

mGluR8

128 nM (EC50)

In Vitro

VU0422288 (1 μM; 5 min) enhances 30 μM LSP4-2022-induced reductions in the field excitatory postsynaptic potentials (fEPSPs) slope on Coronal slices containing the hippocampus[1].
VU0422288 (1 μM; 10 min) can not alter the fEPSP slopes alone, indicating that mGlu7 is not tonically active in Mecp2-/y slices under stimulation conditions[2].

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

In Vivo

VU0422288 (30 mg/kg; i.p.; once daily for 17 days) rescues synaptic plasticity defects and learning and memory phenotypes, reduces the number of apneas in Mecp2+/- mice, while VU0422288 has no effect in Mecp2+/+ animals[2].
VU0422288 (10 mg/kg; i.p.; single dose) exhibis a plasma/brain partitioning coefficient of 1.67 in adult male Sprague-Dawley rats, with predicted unbound brain concentration of about 40 nM[2].

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

Molecular Weight

360.19

Formula

C17H11Cl2N3O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C(NC(C1=CC=CC=N1)=O)C=C2)=C2OC3=CC=C(Cl)C=N3

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 (69.41 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 2.7763 mL 13.8816 mL 27.7631 mL
5 mM 0.5553 mL 2.7763 mL 5.5526 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 mg/mL (6.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.88%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7763 mL 13.8816 mL 27.7631 mL 69.4078 mL
5 mM 0.5553 mL 2.7763 mL 5.5526 mL 13.8816 mL
10 mM 0.2776 mL 1.3882 mL 2.7763 mL 6.9408 mL
15 mM 0.1851 mL 0.9254 mL 1.8509 mL 4.6272 mL
20 mM 0.1388 mL 0.6941 mL 1.3882 mL 3.4704 mL
25 mM 0.1111 mL 0.5553 mL 1.1105 mL 2.7763 mL
30 mM 0.0925 mL 0.4627 mL 0.9254 mL 2.3136 mL
40 mM 0.0694 mL 0.3470 mL 0.6941 mL 1.7352 mL
50 mM 0.0555 mL 0.2776 mL 0.5553 mL 1.3882 mL
60 mM 0.0463 mL 0.2314 mL 0.4627 mL 1.1568 mL
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VU0422288 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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VU0422288
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