2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. VU-29

VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM).

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VU-29 Chemical Structure

VU-29 Chemical Structure

CAS No. : 890764-36-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

VU-29 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM)[1][2].

IC50 & Target

rat mGluR5

9 nM (EC50)

rat mGluR1

557 nM (EC50)

rat mGluR2

1.5 μM (EC50)

hmGluR4

154 nM (EC50)

rat mGluR5

224 nM (Ki)

In Vivo

VU-29 (500 nM) potentiates DHPG induced increases in phosphoinositide (PI) hydrolysis in rat hippocampal slices. VU-29 potentiates threshold TBS-induced long term potentiation (LTP) in rat hippocampal CA1 region. VU-29 (1 µM) potentiates chemically induced mGluR-long term depression (LTD) in area CA1 of the rat hippocampus. VU-29 (1 µM) potentiates stimulus-induced NMDA receptor-independent LTD[1].

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

384.39

Formula

C22H16N4O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC(C2=CC=CC=C2)=NN1C3=CC=CC=C3)C4=CC=C([N+]([O-])=O)C=C4
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 : 50 mg/mL (130.08 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 2.6015 mL 13.0076 mL 26.0152 mL
5 mM 0.5203 mL 2.6015 mL 5.2030 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 5 mg/mL (13.01 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
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 2.6015 mL 13.0076 mL 26.0152 mL 65.0381 mL
5 mM 0.5203 mL 2.6015 mL 5.2030 mL 13.0076 mL
10 mM 0.2602 mL 1.3008 mL 2.6015 mL 6.5038 mL
15 mM 0.1734 mL 0.8672 mL 1.7343 mL 4.3359 mL
20 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2519 mL
25 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6015 mL
30 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1679 mL
40 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
50 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3008 mL
60 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0840 mL
80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8130 mL
100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
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VU-29 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.

Keywords:

VU-29890764-36-0VU29VU 29mGluRMetabotropic glutamate receptorsLTPLTDallostericpotentiatorrathippocampalInhibitorinhibitorinhibit

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