VU0409106
Based on 1 Customer Validation
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.76%
- No. CAS: 1276617-62-9
- Fòrmula: C15H11FN4O2S
- Peso molecular:330.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Actividad biológica
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mGlu5 24 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
49 nM
Compound: 24, VU0409106
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Allosteric modulation of human mGlu5 receptor expressed in HEK cells assessed as effect on glutamate-induced calcium mobilization
Allosteric modulation of human mGlu5 receptor expressed in HEK cells assessed as effect on glutamate-induced calcium mobilization
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[PMID: 24074843] |
| HEK293-A | IC50 |
24 nM
Compound: 24, VU0409106
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Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds
Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds
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[PMID: 24074843] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:10 mg/kg (10% Tween 80 formulation)
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Administration:Intraperitoneal injection.
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Result:
1.19 Pharmacokinetic Parameters of VU0409106 in CD-1 mice[1].
IP (10 mg/kg) Plasma Tmax (h) 0.25 Plasma Cmax (ng/mL) 1450 Brain Tmax (h) 0.25 Brain Cmax (ng/mL) 1350 AUCplasma (ng/mL•h) 702 AUCbrain (ng/mL•h) 696 B/P ratio 0.99
Chemical Information
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No. CAS 1276617-62-9
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Appearance Solid
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Peso molecular 330.34
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Fòrmula C15H11FN4O2S
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Color White to off-white
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SMILES
CC1=CSC(NC(C2=CC(F)=CC(OC3=CN=CN=C3)=C2)=O)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 2 mg/mL (6.05 mM; ultrasonic and warming and heat to 60°C; 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)
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Felts AS, et al. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. [Content Brief]
[2]. Morrison RD, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metab Dispos. 2012 Sep;40(9):1834-45. [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. 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 | 3.0272 mL | 15.1359 mL | 30.2718 mL | 75.6796 mL |
| 5 mM | 0.6054 mL | 3.0272 mL | 6.0544 mL | 15.1359 mL |
VU0409106 Related Classifications
HY-110180 Related Classifications
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