VU 0364439
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.42%
- CAS. Nr.: 1246086-78-1
- Formel: C18H13Cl2N3O3S
- Molecular Weight:422.29
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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mGlu4 Receptor 19.8 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
19.8 nM
Compound: 11
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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
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[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.
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Cell Line:human osteosarcoma MG-63 cells
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Concentration:20 nM
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Incubation Time:48 h
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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.
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Cell Line:human osteosarcoma MG-63 cells
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Concentration:20 nM
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Incubation Time:48 h
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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.
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Cell Line:human osteosarcoma MG-63 cells
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Concentration:20 nM
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Incubation Time:48 h
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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
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CAS. Nr. 1246086-78-1
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Appearance Solid
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Molecular Weight 422.29
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Formel C18H13Cl2N3O3S
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Color White to off-white
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SMILES
O=C(C1=NC=CC=C1)NC2=CC=C(S(=O)(NC3=CC=CC=C3Cl)=O)C(Cl)=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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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)
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Handling Instructions (2659 KB)
Verweise
[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]
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 | 2.3680 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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