JNJ-46778212
Based on 1 Customer Validation
JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 1363281-27-9
- Formula: C20H17FN2O3
- Molecular Weight:352.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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GPCR/G Protein Compound Library
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Neurotransmitter Receptor Compound Library
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
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Highly Selective Activators Library
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Allosteric Modulators (AMs) Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
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mGlu5 Receptor 260 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
235 nM
Compound: 162; VU0409551
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Positive allosteric modulation of rat mGlu5 receptor expressed in HEK293 cells assessed as increase in calcium mobilization
Positive allosteric modulation of rat mGlu5 receptor expressed in HEK293 cells assessed as increase in calcium mobilization
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[PMID: 29939744] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1363281-27-9
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Appearance Solid
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Molecular Weight 352.36
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Formula C20H17FN2O3
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Color Light yellow to yellow
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SMILES
O=C(N1CCC2=C(OC(COC3=CC=CC=C3)=N2)C1)C4=CC=C(F)C=C4
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Synonyms
VU 0409551
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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 : 100 mg/mL (283.80 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.90 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.90 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Protocol
Mice[1]
SR−/− mice receive once daily, intraperitoneal (i.p.) injections of vehicle (20% hydroxypropyl β-cyclodextran) or VU0409551 for 5 days at a volume of 10 mL/kg. For the in vivo pharmacokinetic and dose-finding experiments, WT mice (n=5–6/dose) receive vehicle or VU0409551 (10 and 30 mg/kg). For the SR−/− mice reversal studies, WT mice receive vehicle and SR−/− mice receive either vehicle or VU0409551 (30 mg/kg). All mice are killed 2 h after the last injection on day 5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
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 | 2.8380 mL | 14.1900 mL | 28.3801 mL | 70.9502 mL |
| 5 mM | 0.5676 mL | 2.8380 mL | 5.6760 mL | 14.1900 mL | |
| 10 mM | 0.2838 mL | 1.4190 mL | 2.8380 mL | 7.0950 mL | |
| 15 mM | 0.1892 mL | 0.9460 mL | 1.8920 mL | 4.7300 mL | |
| 20 mM | 0.1419 mL | 0.7095 mL | 1.4190 mL | 3.5475 mL | |
| 25 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8380 mL | |
| 30 mM | 0.0946 mL | 0.4730 mL | 0.9460 mL | 2.3650 mL | |
| 40 mM | 0.0710 mL | 0.3548 mL | 0.7095 mL | 1.7738 mL | |
| 50 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
| 60 mM | 0.0473 mL | 0.2365 mL | 0.4730 mL | 1.1825 mL | |
| 80 mM | 0.0355 mL | 0.1774 mL | 0.3548 mL | 0.8869 mL | |
| 100 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL |
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