VU0422288
Based on 1 Customer Validation
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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- Pureza: 99.94%
- No. CAS: 1630936-95-6
- Fòrmula: C17H11Cl2N3O2
- Peso molecular:360.19
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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mGluR4 108 nM (EC50) |
mGluR7 146 nM (EC50) |
mGluR8 128 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
0.108 μM
Compound: VU0422288; 14
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Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
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[PMID: 30881607] |
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.
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.
Chemical Information
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No. CAS 1630936-95-6
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Appearance Solid
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Peso molecular 360.19
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Fòrmula C17H11Cl2N3O2
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Color White to off-white
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SMILES
ClC(C=C(NC(C1=CC=CC=N1)=O)C=C2)=C2OC3=CC=C(Cl)C=N3
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Synonyms
ML396
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Pureza y Documentación
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Ficha de datos (273 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jalan-Sakrikar N, et al. Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7. ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. [Content Brief]
[2]. Gogliotti RG, et al. mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome. Sci Transl Med. 2017 Aug 16;9(403):eaai7459. [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, 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 |
VU0422288 Related Classifications
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