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About This Item
Empirical Formula (Hill Notation):
C22H25FN4O
CAS Number:
Molecular Weight:
380.46
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
NA-014 is a brain-penetrant piperazinyl-acetamide that functions as a highly selective positive allosteric modulator (PAM) of the excitatory amino acid transporter 2 (EAAT2), with no activity on EAAT1 and EAAT3. NA-014 effectively enhances EAAT2-mediated glutamate uptake, demonstrating an EC50 of 3.5 nM and an efficacy of 167.3% in EAAT1−3 transfected COS-7 cells, and an EC50 of 13.4 nM with 189.4% efficacy in glial cultures. NA-014 does not exhibit off-target effects on a broad panel of related receptors, including the hERG channel, displays good metabolic stability, possesses moderate water solubility, and shows favorable pharmacokinetic properties. Additionally, both enantiomers of NA-014 are active, binding at the allosteric site of human EAAT2 and demonstrating equivalent activity in functional assays designed to assess stimulation of EAAT2.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Skin Irrit. 2
Storage Class
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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