VU0364289
Based on 1 Customer Validation
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.52%
- CAS No.: 1242443-29-3
- Formule: C20H21N3O2
- Masse moléculaire:335.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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GPCR/G Protein Compound Library
HY-L006
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Neuronal Signaling Compound Library
HY-L013
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CNS-Penetrant Compound Library
HY-L028
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Neurotransmitter Receptor Compound Library
HY-L062
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Activators Library
HY-L159
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Allosteric Modulators (AMs) Compound Library
HY-L170
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Activité biologique
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mGlu5 1.6 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
1.6 μM
Compound: 10e, VU0364289
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Positive allosteric modulation at rat mGluR5 receptor expressed in HEK293 cells assessed as glutamate-induced calcium fluorescence by Fluo-4/AM dye-based fluorescence assay
Positive allosteric modulation at rat mGluR5 receptor expressed in HEK293 cells assessed as glutamate-induced calcium fluorescence by Fluo-4/AM dye-based fluorescence assay
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[PMID: 23308336] |
VU0364289 (10 mg/kg; i.p.; once) is rapidly and significantly absorbed in rats, and shows excellent central nervous system penetration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (250-275 g)[1].
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Dosage:10, 30, 56.6, 100 mg/kg
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Administration:Intraperitoneal injection; once.
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Result:Showed activity of reversing the hyperlocomotion induced by amphetamine, and can also significantly fewer ambulations in rats when dose up to 56.6 mg/kg.
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Animal Model:Adult male Sprague-Dawley rats (250-275 g)[1].
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; once.
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Result:
1.19 Pharmacokinetic Parameters of VU0364289 in male Sprague-Dawley rats[1].
Tmax (h) Cmax (ng/mL) Plasma protein binding Rat Fu (free fraction) IP (10 mg/kg) 0.25 1280 94% (h); 90% (r) 0.10
Chemical Information
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CAS No. 1242443-29-3
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Appearance Solid
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Masse moléculaire 335.40
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Formule C20H21N3O2
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Color Yellow to brown
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SMILES
N#CC1=CC=CC=C1N2CCN(CC2)C(COCC3=CC=CC=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (298.15 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. 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. 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 (7.45 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.45 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 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.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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. 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 |
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| DMSO | 1 mM | 2.9815 mL | 14.9076 mL | 29.8151 mL | 74.5379 mL |
| 5 mM | 0.5963 mL | 2.9815 mL | 5.9630 mL | 14.9076 mL | |
| 10 mM | 0.2982 mL | 1.4908 mL | 2.9815 mL | 7.4538 mL | |
| 15 mM | 0.1988 mL | 0.9938 mL | 1.9877 mL | 4.9692 mL | |
| 20 mM | 0.1491 mL | 0.7454 mL | 1.4908 mL | 3.7269 mL | |
| 25 mM | 0.1193 mL | 0.5963 mL | 1.1926 mL | 2.9815 mL | |
| 30 mM | 0.0994 mL | 0.4969 mL | 0.9938 mL | 2.4846 mL | |
| 40 mM | 0.0745 mL | 0.3727 mL | 0.7454 mL | 1.8634 mL | |
| 50 mM | 0.0596 mL | 0.2982 mL | 0.5963 mL | 1.4908 mL | |
| 60 mM | 0.0497 mL | 0.2485 mL | 0.4969 mL | 1.2423 mL | |
| 80 mM | 0.0373 mL | 0.1863 mL | 0.3727 mL | 0.9317 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7454 mL |
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