VU0483605
Based on 1 Customer Validation
VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively.
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- Pureza: 97.30%
- No. CAS: 1623101-11-0
- Fòrmula: C20H10Cl3N3O3
- Peso molecular:446.67
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Actividad biológica
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Human mGluR1 390 nM (EC50) |
rat mGluR1 356 nM (EC50) |
Human mGlu4 >10 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
390 nM
Compound: 8
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Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
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[PMID: 26426481] |
VU0483605 proves superior with excellent mGlu1 PAM activity at both human (EC50 = 390 nM) and rat (EC50 = 356 nM, pEC50 = 6.45 ± 0.11, 113 ± 5% Glu Max) and no activity as an mGlu4 PAM (EC50 >10 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1623101-11-0
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Appearance Solid
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Peso molecular 446.67
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Fòrmula C20H10Cl3N3O3
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Color Light yellow to orange
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SMILES
O=C(C1=NC=CC=C1Cl)NC2=CC=C(N(C(C3=C4C=CC=C3Cl)=O)C4=O)C(Cl)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 100 mg/mL (223.88 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 (protect from light). 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 (protect from light). 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.60 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (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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Instrucciones de manejo (2659 KB)
Referencias
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 (protect from light). 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 | 2.2388 mL | 11.1939 mL | 22.3879 mL | 55.9697 mL |
| 5 mM | 0.4478 mL | 2.2388 mL | 4.4776 mL | 11.1939 mL | |
| 10 mM | 0.2239 mL | 1.1194 mL | 2.2388 mL | 5.5970 mL | |
| 15 mM | 0.1493 mL | 0.7463 mL | 1.4925 mL | 3.7313 mL | |
| 20 mM | 0.1119 mL | 0.5597 mL | 1.1194 mL | 2.7985 mL | |
| 25 mM | 0.0896 mL | 0.4478 mL | 0.8955 mL | 2.2388 mL | |
| 30 mM | 0.0746 mL | 0.3731 mL | 0.7463 mL | 1.8657 mL | |
| 40 mM | 0.0560 mL | 0.2798 mL | 0.5597 mL | 1.3992 mL | |
| 50 mM | 0.0448 mL | 0.2239 mL | 0.4478 mL | 1.1194 mL | |
| 60 mM | 0.0373 mL | 0.1866 mL | 0.3731 mL | 0.9328 mL | |
| 80 mM | 0.0280 mL | 0.1399 mL | 0.2798 mL | 0.6996 mL | |
| 100 mM | 0.0224 mL | 0.1119 mL | 0.2239 mL | 0.5597 mL |
VU0483605 Related Classifications
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