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
Biological Activity
Description
IC50 & Target
[1]|
EAAT2 |
In Vitro
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.
Parmacokinetics
| 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
In Vitro:
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)
In Vivo:
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 (6.57 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 (6.57 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (271 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 |
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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 |
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