VU6012962
Based on 1 Customer Validation
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 2313526-86-0
- Formula: C21H19F3N4O4
- Molecular Weight:448.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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mGlu7 347 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6J male mice (8 weeks old)[1]
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Dosage:1, 3, and 10 mg/kg
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Administration:I.p. injections; 60 minutes prior to testing
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Result:Increased total time spent in the open arms at a dose of 3 mg/kg. 10 mg/kg did cause a decrease in overall locomotion.
Chemical Information
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CAS No. 2313526-86-0
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Appearance Solid
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Molecular Weight 448.40
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Formula C21H19F3N4O4
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Color White to light yellow
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SMILES
O=C(C1=CC=C(OCC2CC2)C(OC)=C1)NC3=C(N4C=NC=N4)C=CC(OC(F)(F)F)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 125 mg/mL (278.77 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, 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.
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.
Purity & Documentation
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Data Sheet (274 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)
References
[1]. Reed CW, et al. Discovery of an orally bioavailable and Central Nervous System (CNS) penetrant mGlu7 NegativeAllosteric Modulator (NAM) in vivo tool compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962). J Med Chem. 2019 Jan 4. [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 | 2.2302 mL | 11.1508 mL | 22.3015 mL | 55.7538 mL |
| 5 mM | 0.4460 mL | 2.2302 mL | 4.4603 mL | 11.1508 mL | |
| 10 mM | 0.2230 mL | 1.1151 mL | 2.2302 mL | 5.5754 mL | |
| 15 mM | 0.1487 mL | 0.7434 mL | 1.4868 mL | 3.7169 mL | |
| 20 mM | 0.1115 mL | 0.5575 mL | 1.1151 mL | 2.7877 mL | |
| 25 mM | 0.0892 mL | 0.4460 mL | 0.8921 mL | 2.2302 mL | |
| 30 mM | 0.0743 mL | 0.3717 mL | 0.7434 mL | 1.8585 mL | |
| 40 mM | 0.0558 mL | 0.2788 mL | 0.5575 mL | 1.3938 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4460 mL | 1.1151 mL | |
| 60 mM | 0.0372 mL | 0.1858 mL | 0.3717 mL | 0.9292 mL | |
| 80 mM | 0.0279 mL | 0.1394 mL | 0.2788 mL | 0.6969 mL | |
| 100 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5575 mL |