1. Membrane Transporter/Ion Channel
  2. EAAT
  3. 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.

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NA-014

NA-014 화학구조

CAS No. : 3041127-59-4

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

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  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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.

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 %
분자량

380.46

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

용액&용해도
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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
순도&문서

Purity: 99.49%

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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  • 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.

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Inquiry Information

상품명:
NA-014
Cat. No.:
HY-162455
수량:
MCE Japan Authorized Agent: