VU 0357121
Based on 1 Customer Validation
VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.73%
- CAS. Nr.: 433967-28-3
- Formel: C17H17F2NO2
- Molecular Weight:305.32
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-70059
LY341495mGluR Antagonist -
HY-14609
MPEP HydrochloridemGlu5 Receptor Antagonist -
HY-13206
MTEP hydrochloridemGlu5 Antagonist -
HY-14609A
MPEPmGlu5 Receptor Antagonist -
HY-14612
CPPHAmGluR5/mGluR1 Modulator -
HY-15446
BasimglurantmGlu5 Negative Allosteric Modulator -
HY-15445
CTEPmGluR Antagonist -
HY-13239
LY2979165mGluR Receptor Agonist -
HY-14859
DipraglurantmGluR5 NAM -
HY-N0390
L-GlutamineEndogenous Metabolite -
HY-13058
ADX-47273mGluR5 PAM -
HY-N0390R
L-Glutamine (Standard)Reference Standard
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
mGlu5 Receptor 33 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
33 nM
Compound: 6, VU0357121
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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] |
In Vitro
VU 0357121 has the ability to enhance glutamate sensitivity of mGlu5 is likely due to the interaction at a site on the receptor distinct from the MPEP binding site. VU 0357121 does not bind at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU 0357121 to shift the glutamate concentration response curve, whereas the response to VU 0357121 is not altered by the F585I/rmGlu5 mutation. VU 0357121 shows weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 433967-28-3
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Appearance Solid
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Molecular Weight 305.32
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Formel C17H17F2NO2
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Color White to off-white
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SMILES
O=C(NC1=CC=C(F)C=C1F)C2=CC=C(OCCCC)C=C2
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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 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 50 mg/mL (163.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.19 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
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 (459 KB)
- English - EN (459 KB)
- Français - FR (459 KB)
- Deutsch - DE (459 KB)
- Norwegian - NO (459 KB)
- Español - ES (459 KB)
- Swedish - SV (459 KB)
- Italian - IT (459 KB)
- Korean - KR (459 KB)
- Portuguese - PT (459 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 3.2753 mL | 16.3763 mL | 32.7525 mL | 81.8813 mL |
| 5 mM | 0.6551 mL | 3.2753 mL | 6.5505 mL | 16.3763 mL | |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2753 mL | 8.1881 mL | |
| 15 mM | 0.2184 mL | 1.0918 mL | 2.1835 mL | 5.4588 mL | |
| 20 mM | 0.1638 mL | 0.8188 mL | 1.6376 mL | 4.0941 mL | |
| 25 mM | 0.1310 mL | 0.6551 mL | 1.3101 mL | 3.2753 mL | |
| 30 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7294 mL | |
| 40 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0470 mL | |
| 50 mM | 0.0655 mL | 0.3275 mL | 0.6551 mL | 1.6376 mL | |
| 60 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3647 mL | |
| 80 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 100 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL |
VU 0357121 Related Classifications
HY-15393 Related Classifications
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