VU 0364439

Alias: VU0364439, VU-0364439, VU 0364439

Cat No.:V1085 Purity: ≥98%

COA Product Data Instructions for use SDS

VU 0364439 (VU0364439; VU-0364439) is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with important biological activity.

VU 0364439 Chemical Structure CAS No.: 1246086-78-1
Product category: GluR

This product is for research use only, not for human use. We do not sell to patients.

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10mg
25mg
50mg
100mg
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Nature 2021, 597(7874):119-125.

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Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

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Science Trans Med 2023, 15: eadd7872.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

VU 0364439 (VU0364439; VU-0364439) is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with important biological activity. It inhibits mGlu4 with an EC50 value of 19.8 nM. Due to the fact that VU 0364439 possessed less favorable pharmacokinetic properties, thus it can not be used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds. The activation of the mGlu4 receptor, either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

In vitro activity: VU 0364439 is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with EC50 value of 19.8 nM. VU 0364439 possessed less favorable pharmacokinetic properties. The properties of VU 0364439 prevents VU 0364439 itself from being used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds. The activation of the mGlu4 receptor, either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinsons disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons.

Kinase Assay: VU 0364439 is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with EC50 value of 19.8 nM.

Cell Assay: VU 0364439 exhibited excellent in vitro maximal response and potency relative to another PAM, (−)-PHCCC (a partially selective mGlu4 potentiator, its chemical structure could be found in reference 4). Starting at 30µM, using a 1:3 serial dilutions, VU 0364439 was tested in triplicate. The entire test was performed on one day. Finally, the % (−)-PHCCC value of VU 0364439 was 102.3. The value of % (−)-PHCCC was computed through dividing the maximal response elicited by VU 0364439 by the response of the control PAM, (−)-PHCCC, on the same day. It was also found that the EC50 value of VU 0364439 was 19.8 nM at human mGlu4

ln Vivo

VU 0364439 possess less than ideal PK properties preventing their use as in vivo tools. It shows better stability in HLM (63% remaining) than RLM (2% remaining).

Animal Protocol

N/A

References

Bioorg Med Chem Lett.2010 Sep 1;20(17):5175-8;J Med Chem.2011 Jul 28;54(14):5070-81.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C18H13CL2N3O3S

Molecular Weight

422.29

CAS #

1246086-78-1

Related CAS #

1246086-78-1

SMILES

O=C(C1=NC=CC=C1)NC2=CC=C(S(=O)(NC3=CC=CC=C3Cl)=O)C(Cl)=C2

Synonyms

VU0364439, VU-0364439, VU 0364439

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 85 mg/mL (201.3 mM)

Water:<1 mg/mL

Ethanol:<1 mg/mL

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3680 mL	11.8402 mL	23.6804 mL
	5 mM	0.4736 mL	2.3680 mL	4.7361 mL
	10 mM	0.2368 mL	1.1840 mL	2.3680 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Concentration-dependent potentiation of glutamate in mGlu4/Gqi5 CHO cells by 5. In the absence of an EC20 concentration of glutamate, 5, does not elicit receptor activation.Bioorg Med Chem Lett.2010 Sep 1;20(17):5175-8.

HTS Hit (VU0130734,4) to lead (VU0361591,5).Bioorg Med Chem Lett.2010 Sep 1;20(17):5175-8.