NA-014
Based on 1 Customer Validation
NA-014 is an excitatory amino acid transporter 2 (EAAT2)-selective positive allosteric modulator. NA-014 increases EAAT2-mediated glutamate uptake. NA-014 can be used for the research of epilepsy, neuropathic pain, stroke, drugs of abuse disorders.
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 3041127-59-4
- Formula: C22H25FN4O
- Molecular Weight:380.46
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Highly Selective Activators Library
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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
Biological Activity
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EAAT2 |
NA-014 (0.00001-10000 nM) potently and selectively acts as a positive allosteric modulator of EAAT2 in EAAT2-expressing COS-7 cells, with an EC50 of 3.0 nM, and has no effect on EAAT1 or EAAT3[1].
NA-014 (10-500 nM) increases the Vmax of EAAT2-mediated L-glutamate uptake in EAAT2-expressing COS-7 cells[1].
NA-014 (0.00001-10000 nM) acts as a positive allosteric modulator of endogenous EAATs in primary glia cultures, with an EC50 of 13.4 nM[1].
NA-014 (10-500 nM) increases the Vmax of endogenous EAAT-mediated L-glutamate uptake in primary glia cultures[1].
NA-014 exhibits good metabolic stability in mouse liver microsomes, moderate aqueous solubility, and modest hERG channel binding affinity[1].
NA-014 is highly selective for EAAT2, with no detectable off-target activity against a broad panel of neurotransmitter transporters, glutamate receptors, and other receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax (Plasma) | Cmax | T1/2 (Plasma) | AUC0-∞ (Plasma) | Cmax (Brain) | T1/2 (Brain) | AUC0-∞ (Brain) | Brain-to-Plasma Ratio |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 0.500 h | 330 ng/mL | 1.19 h | 624 ng·h/mL | 279 ng/mL | 1.23 h | 515 ng·h/mL | 132 % |
Chemical Information
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CAS No. 3041127-59-4
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Appearance Solid
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Molecular Weight 380.46
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Formula C22H25FN4O
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Color Light yellow to brown
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SMILES
O=C(NCCC1=CC=C(F)C=C1)C(C2=CC=C(C#N)C=C2)N3CCN(C)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (262.84 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (270 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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Handling Instructions (2659 KB)
References
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 (stored under nitrogen). 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 | 2.6284 mL | 13.1420 mL | 26.2840 mL | 65.7099 mL |
| 5 mM | 0.5257 mL | 2.6284 mL | 5.2568 mL | 13.1420 mL | |
| 10 mM | 0.2628 mL | 1.3142 mL | 2.6284 mL | 6.5710 mL | |
| 15 mM | 0.1752 mL | 0.8761 mL | 1.7523 mL | 4.3807 mL | |
| 20 mM | 0.1314 mL | 0.6571 mL | 1.3142 mL | 3.2855 mL | |
| 25 mM | 0.1051 mL | 0.5257 mL | 1.0514 mL | 2.6284 mL | |
| 30 mM | 0.0876 mL | 0.4381 mL | 0.8761 mL | 2.1903 mL | |
| 40 mM | 0.0657 mL | 0.3285 mL | 0.6571 mL | 1.6427 mL | |
| 50 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL | 1.3142 mL | |
| 60 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 80 mM | 0.0329 mL | 0.1643 mL | 0.3285 mL | 0.8214 mL | |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6571 mL |
NA-014 Related Classifications
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