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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.49%
- CAS 番号: 3041127-59-4
- 分子式: C22H25FN4O
- 分子量:380.46
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保管条件:
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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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
生物活性
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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 % |
化学情報
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CAS 番号 3041127-59-4
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性状 Solid
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分子量 380.46
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 |
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| 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 関連分類
HY-162455 関連分類
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