Cat. No.: HY-15476

VU 0364439

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VU 0364439 is a mGlu4 positive allosteric modulator with an EC₅₀ of 19.8 nM. VU 0364439 modulates the GRM4/CBX4/HIF-1α signaling pathway by enhancing GRM4-CBX4 interaction. VU 0364439 can be used for the research of parkinson’s disease.

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Pureté: 99.42%
CAS No.: 1246086-78-1
Formule: C₁₈H₁₃Cl₂N₃O₃S
Masse moléculaire:422.29

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

VU 0364439 Chemical Structure

CAS No.: 1246086-78-1

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

mGlu4 Receptor

19.8 nM (EC₅₀)

Voir tous les produits spécifiques à Isoform mGluR :

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase :

Voir tous les produits spécifiques à Isoform VEGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	19.8 nM Compound: 11	Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization	[PMID: 20667732]

In Vitro

VU 0364439 potently potentiates glutamate-mediated calcium mobilization in BHK cells stably expressing human mGlu4 and murine GR15, with an EC₅₀ of 20 nM^[1].
VU 0364439 (20 nM; 48 h) has no independent effect on GRM4 expression or the HIF-1α pathway, but significantly enhances the GRM4 overexpression-induced reduction in VEGFA and PDK1 levels in human osteosarcoma MG-63 cells^[2].
VU 0364439 (20 nM) has no independent inhibitory effect on cell proliferation, but significantly enhances the GRM4 overexpression-induced inhibition of this malignant cell behavior in human osteosarcoma MG-63 cells^[2].
VU 0364439 (20 nM; 48 h) has no independent inhibitory effect on cell migration and invasion, but significantly enhances the GRM4 overexpression-induced inhibition of this malignant cell behavior in human osteosarcoma MG-63 cells^[2].
VU 0364439 is highly protein bound, with a free fraction of 0.1% in both rat and human biological matrices^[3].

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

Real Time qPCR^[2]

Cell Line:

human osteosarcoma MG-63 cells
Concentration:

20 nM
Incubation Time:

48 h
Result:

Exhibited no significant effect on GRM4 expression, or on the mRNA and protein levels of HIF-1α downstream targets VEGFA and PDK1.
Caused a significantly greater reduction in VEGFA and PDK1 mRNA and protein levels when combined with GRM4 overexpression compared to GRM4 overexpression alone.
Increased GRM4 expression, while leaving CBX4 and HIF-1α expression unchanged when combined with GRM4 overexpression.

Cell Migration Assay ^[2]

Cell Line:

human osteosarcoma MG-63 cells
Concentration:

20 nM
Incubation Time:

48 h
Result:

Exhibited no significant inhibitory effect on MG-63 cell migration.
Caused a significantly greater inhibition of cell migration when combined with GRM4 overexpression compared to GRM4 overexpression alone.

Cell Invasion Assay^[2]

Cell Line:

human osteosarcoma MG-63 cells
Concentration:

20 nM
Incubation Time:

48 h
Result:

Exhibited no significant inhibitory effect on MG-63 cell invasion.
Caused a significantly greater inhibition of cell invasion when combined with GRM4 overexpression compared to GRM4 overexpression alone.

Chemical Information

CAS No. 1246086-78-1
Appearance Solid
Masse moléculaire 422.29
Formule C₁₈H₁₃Cl₂N₃O₃S
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (118.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (5.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.92 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Hong SP, et al. Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. J Med Chem. 2011;54(14):5070-5081. [Content Brief]

[2]. Zhang Z, et al. GRM4 inhibits the proliferation, migration, and invasion of human osteosarcoma cells through interaction with CBX4. Biosci Biotechnol Biochem. 2020;84(2):279-289. [Content Brief]

[3]. Engers DW, et al. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorg Med Chem Lett. 2010;20(17):5175-5178. [Content Brief]

[4]. Robichaud AJ, et al. Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics. ACS Chem Neurosci. 2011;2(8):433-449. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.3680 mL	11.8402 mL	23.6804 mL	59.2010 mL
	5 mM	0.4736 mL	2.3680 mL	4.7361 mL	11.8402 mL
	10 mM	0.2368 mL	1.1840 mL	2.3680 mL	5.9201 mL
	15 mM	0.1579 mL	0.7893 mL	1.5787 mL	3.9467 mL
	20 mM	0.1184 mL	0.5920 mL	1.1840 mL	2.9601 mL
	25 mM	0.0947 mL	0.4736 mL	0.9472 mL	2.3680 mL
	30 mM	0.0789 mL	0.3947 mL	0.7893 mL	1.9734 mL
	40 mM	0.0592 mL	0.2960 mL	0.5920 mL	1.4800 mL
	50 mM	0.0474 mL	0.2368 mL	0.4736 mL	1.1840 mL
	60 mM	0.0395 mL	0.1973 mL	0.3947 mL	0.9867 mL
	80 mM	0.0296 mL	0.1480 mL	0.2960 mL	0.7400 mL
	100 mM	0.0237 mL	0.1184 mL	0.2368 mL	0.5920 mL

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VU 0364439

Bioactive Compound Library Max

Bioactive Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

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Metabolic Enzyme Compound Library

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Anti-Hematopathy Compound Library

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Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform mGluR

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase

Voir tous les produits spécifiques à Isoform VEGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

VU 0364439 Related Classifications

HY-15476 Related Classifications