VU0360172
Based on 1 Customer Validation
VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice. VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Reinheit : 98.07%
- CAS. Nr.: 1310012-12-4
- Formel: C18H15FN2O
- Molecular Weight:294.32
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
mGluR5 16 nM (EC50) |
mGluR5 195 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
39 nM
Compound: 26, VU0360172
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Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as calcium mobilization
Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as calcium mobilization
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[PMID: 24050755] |
| HEK293 | EC50 |
16 nM
Compound: 3, VU0360172
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Positive allosteric modulation of rat mGluR5 expressed in human HEK293 cells assessed as calcium mobilization
Positive allosteric modulation of rat mGluR5 expressed in human HEK293 cells assessed as calcium mobilization
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[PMID: 22981332] |
Chemical Information
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CAS. Nr. 1310012-12-4
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Appearance Solid
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Molecular Weight 294.32
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Formel C18H15FN2O
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Color Light yellow to brown
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SMILES
O=C(NC1CCC1)C2=CC=C(N=C2)C#CC3=CC=CC(F)=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 83.33 mg/mL (283.13 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
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Data Sheet (269 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]. Alice L Rodriguez, et al. Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol Pharmacol. 2010 Dec;78(6):1105-23. [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 (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 | 3.3977 mL | 16.9883 mL | 33.9766 mL | 84.9416 mL |
| 5 mM | 0.6795 mL | 3.3977 mL | 6.7953 mL | 16.9883 mL | |
| 10 mM | 0.3398 mL | 1.6988 mL | 3.3977 mL | 8.4942 mL | |
| 15 mM | 0.2265 mL | 1.1326 mL | 2.2651 mL | 5.6628 mL | |
| 20 mM | 0.1699 mL | 0.8494 mL | 1.6988 mL | 4.2471 mL | |
| 25 mM | 0.1359 mL | 0.6795 mL | 1.3591 mL | 3.3977 mL | |
| 30 mM | 0.1133 mL | 0.5663 mL | 1.1326 mL | 2.8314 mL | |
| 40 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1235 mL | |
| 50 mM | 0.0680 mL | 0.3398 mL | 0.6795 mL | 1.6988 mL | |
| 60 mM | 0.0566 mL | 0.2831 mL | 0.5663 mL | 1.4157 mL | |
| 80 mM | 0.0425 mL | 0.2124 mL | 0.4247 mL | 1.0618 mL | |
| 100 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8494 mL |
VU0360172 Related Classifications
HY-120589 Related Classifications
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