VU0650786
Based on 2 publication(s) in Google Scholar
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.55%
- CAS. Nr.: 1809085-30-0
- Formel: C18H15ClFN5O2
- Molecular Weight:387.80
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Publications Citing Use of MedChemExpress (MCE) VU0650786
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Biologische Aktivität
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mGluR3 392 nM (IC50) |
The pharmacokinetic parameters of VU0650786 (compound 106) in rats[1].
| Parameters | IV (0.2 mg/kg) |
| t1/2 (min) | 42 |
| CL plasma (mL/min/kg) | 37 |
| VSS (L/kg) | 1.6 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1809085-30-0
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Appearance Solid
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Molecular Weight 387.80
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Formel C18H15ClFN5O2
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Color White to off-white
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SMILES
ClC1=CN=C(OCC2=NN([C@H](C)CN(C3=C(F)N=CC=C3)C4=O)C4=C2)C=C1
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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 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Res
2025 Mar;35(3):165-185. PMID: 39875551 -
eNeuro
Adaptive changes in group-II metabotropic glutamate receptors underlie the deficit in recognition memory induced by methamphetamine in mice. [Abstract]2024 Jul 5:ENEURO.0523-23.2024. PMID: 38969501
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (644.66 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (5.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Engers JL, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem. 2015 Sep 24;58(18):7485-500. [Content Brief]
[2]. Max E Joffe, et al. mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects. Neuron. 2020 Jan 8;105(1):46-59.e3. [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 | 2.5786 mL | 12.8932 mL | 25.7865 mL | 64.4662 mL |
| 5 mM | 0.5157 mL | 2.5786 mL | 5.1573 mL | 12.8932 mL | |
| 10 mM | 0.2579 mL | 1.2893 mL | 2.5786 mL | 6.4466 mL | |
| 15 mM | 0.1719 mL | 0.8595 mL | 1.7191 mL | 4.2977 mL | |
| 20 mM | 0.1289 mL | 0.6447 mL | 1.2893 mL | 3.2233 mL | |
| 25 mM | 0.1031 mL | 0.5157 mL | 1.0315 mL | 2.5786 mL | |
| 30 mM | 0.0860 mL | 0.4298 mL | 0.8595 mL | 2.1489 mL | |
| 40 mM | 0.0645 mL | 0.3223 mL | 0.6447 mL | 1.6117 mL | |
| 50 mM | 0.0516 mL | 0.2579 mL | 0.5157 mL | 1.2893 mL | |
| 60 mM | 0.0430 mL | 0.2149 mL | 0.4298 mL | 1.0744 mL | |
| 80 mM | 0.0322 mL | 0.1612 mL | 0.3223 mL | 0.8058 mL | |
| 100 mM | 0.0258 mL | 0.1289 mL | 0.2579 mL | 0.6447 mL |
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