VU6066098
Based on 1 Customer Validation
VU6066098 is a blood-brain barrier penetrant, orally active inhibitor of metabotropic glutamate receptor subtype 2 (mGlu2), with IC50 values of 77 nM and 111 nM against human and rat targets, respectively. VU6066098 induces antidepressant-like activity, inhibits psychosis-like hyperlocomotion, enhances recognition memory and associative learning, and reverses cognitive deficits caused by blast-related traumatic brain injury. VU6066098 can be used in research on major depressive disorder, schizophrenia, Alzheimer's disease, and traumatic brain injury.
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- Pureté : 99.82%
- CAS No.: 3055537-47-5
- Formule: C19H15F2N3O
- Masse moléculaire:339.34
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
VU6066098 inhibits human mGlu2 receptor activity in a cAMP assay with an IC50 of 114 nM[1].
VU6066098 potently inhibits rat mGlu2 receptors with an IC50 of 111 nM, while showing no significant activity against most other rat mGlu receptor subtypes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
VU6066098 (5.6-56.6 mg/kg; p.o.; single dose) exhibits antipsychotic-like activity in rats with an oral minimum effective dose of 30 mg/kg, reversing amphetamine-induced hyperlocomotion in a dose-dependent manner[1].
VU6066098 (1-10 mg/kg; p.o.; single dose) enhances long-term recognition memory in rats with an oral minimum effective dose of 3 mg/kg, producing a robust improvement in recognition index[1].
VU6066098 (0.1-1 mg/kg; p.o.; single dose) enhances associative learning and long-term memory in rats with an oral minimum effective dose of 0.3 mg/kg, increasing percent freezing behavior in contextual fear conditioning[1].
VU6066098 (10 mg/kg; i.p.; daily; 2 days) reverses cognitive deficits in a rat blast-related TBI model when administered at 10 mg/kg i.p. for 2 days, with effects lasting up to 30 days post-dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Reduced immobility time in a dose-dependent manner, with significant effects at all tested doses compared to vehicle.
Reached total brain levels of 230 nM (2.1-fold the rat mGlu2 IC50) and free brain levels of 3.1 nM (0.03-fold the rat mGlu2 IC50) at 1 mg/kg p.o.
Reached total brain levels of 4.9 μM (43.9-fold the rat mGlu2 IC50) and free brain levels of 67 nM (0.59-fold the rat mGlu2 IC50) at 10 mg/kg p.o., with efficacy comparable to 10 mg/kg s.c. ketamine.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:5.6 mg/kg; 10 mg/kg; 30 mg/kg; 56.6 mg/kg
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Administration:p.o.; single dose
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Result:Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, with significant effects at 30 mg/kg and 56.6 mg/kg p.o.
Produced total brain levels of 12.9 μM and free brain levels of 174 nM (1.55-fold the rat mGlu2 IC50) at 30 mg/kg p.o.
Reached total brain levels of 14.9 μM and free brain levels of 202 nM (1.79-fold the rat mGlu2 IC50) at 56.6 mg/kg p.o., with efficacy magnitude comparable to the positive control VU0467154.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Enhanced recognition memory in a dose-dependent manner, with significant increases in recognition index observed at 3 mg/kg and 10 mg/kg p.o.
Produced total brain levels of 1.2 μM (10.5-fold the rat mGlu2 IC50) and free brain levels of 15.9 nM (0.14-fold the rat mGlu2 IC50) at 3 mg/kg p.o.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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Result:Enhanced acquisition of contextual fear conditioning in a dose-dependent manner, with significant increases in percent freezing observed at 0.3 mg/kg and 1 mg/kg p.o.
Produced total brain levels of 46 nM (0.41-fold the rat mGlu2 IC50) and free brain levels of 0.62 nM (0.005-fold the rat mGlu2 IC50) at 0.3 mg/kg p.o.
Reached total brain levels of 318 nM (2.83-fold the rat mGlu2 IC50) and free brain levels of 4.29 nM (0.038-fold the rat mGlu2 IC50) at 1 mg/kg p.o.
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Animal Model:unspecified[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 2 days
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Result:Reversed blast-induced deficits in novel object recognition for both short-term and long-term memory, with significant improvements in discrimination index compared to vehicle-treated blast-exposed rats.
Sustained the memory-enhancing effect for at least 30 days after the last dose administration.
Chemical Information
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CAS No. 3055537-47-5
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Appearance Solid
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Masse moléculaire 339.34
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Formule C19H15F2N3O
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Color White to off-white
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SMILES
FC1=CC(F)=CC=C1C2=CC3=C(CNC3=O)C(C4=CC(C)=NN4C)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (147.34 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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 (sealed storage, away from moisture). 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 | 2.9469 mL | 14.7345 mL | 29.4690 mL | 73.6724 mL |
| 5 mM | 0.5894 mL | 2.9469 mL | 5.8938 mL | 14.7345 mL | |
| 10 mM | 0.2947 mL | 1.4734 mL | 2.9469 mL | 7.3672 mL | |
| 15 mM | 0.1965 mL | 0.9823 mL | 1.9646 mL | 4.9115 mL | |
| 20 mM | 0.1473 mL | 0.7367 mL | 1.4734 mL | 3.6836 mL | |
| 25 mM | 0.1179 mL | 0.5894 mL | 1.1788 mL | 2.9469 mL | |
| 30 mM | 0.0982 mL | 0.4911 mL | 0.9823 mL | 2.4557 mL | |
| 40 mM | 0.0737 mL | 0.3684 mL | 0.7367 mL | 1.8418 mL | |
| 50 mM | 0.0589 mL | 0.2947 mL | 0.5894 mL | 1.4734 mL | |
| 60 mM | 0.0491 mL | 0.2456 mL | 0.4911 mL | 1.2279 mL | |
| 80 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9209 mL | |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2947 mL | 0.7367 mL |
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