2. Membrane Transporter/Ion Channel
  3. EAAT
  4. NA-014

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.

NA-014

NA-014 Chemical Structure

CAS No. : 3041127-59-4

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10 mM * 1 mL in DMSO
ready for reconstitution
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NA-014 Related Antibodies

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Description

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[1].

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.

NA-014 Related Antibodies
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 %
Molecular Weight

380.46

Formula

C22H25FN4O
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

O=C(NCCC1=CC=C(F)C=C1)C(C2=CC=C(C#N)C=C2)N3CCN(C)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6284 mL 13.1420 mL 26.2840 mL
5 mM 0.5257 mL 2.6284 mL 5.2568 mL
View the 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.

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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 99.49%

SDS (251 KB)

COA (245 KB) HNMR (256 KB) LCMS (107 KB)

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
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NA-014 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NA-0143041127-59-4NA014NA 014EAATExcitatory amino acid transporter Glutamate transporter| strokeprimary glia culturesEAAT2mouse liver microsomesblood-brain barrierdrugs of abuse disordersepilepsyglutamate uptakeneuropathic painCOS-7 cellsInhibitorinhibitorinhibit

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