SML4263

NA-014

≥98% (HPLC)

• Synonym(e): 2-(4-Cyanophenyl)-N-(4-fluorophenethyl)-2-(4-methylpiperazin-1-yl)acetamide
• Empirische Formel (Hill-System): C₂₂H₂₅FN₄O
• CAS-Nummer: 3041127-59-4
• Molekulargewicht: 380.46
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C

Beschreibung

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.

Sicherheitshinweise

• Piktogramme: GHS07
• Signalwort: Warning
• Gefahrencodes: H302,H315
• Sicherheitshinweise: P264 - P280 - P301 + P312 - P302 + P352 - P332 + P313 - P362 + P364
• Hazard Classifications: Acute Tox. 4 Oral - Skin Irrit. 2
• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable