F3288-0031
F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferential NET/SERT inhibition with pIC50 = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions.
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- CAS No.: 926493-93-8
- Formule: C24H32N2O3
- Masse moléculaire:396.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
| Species | Dose | Route | Plasma Concentration | Brain Concentration |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 8.31 μM | 52.2 μM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (6-8 weeks)[1]
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Dosage:3, 10, 30, 50 mg/kg
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Administration:i.p., once
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Result:Demonstrated a dose-dependent decrease in immobility time in the forced swim test (FST), with significant reductions at 30 and 50 mg/kg.
Did not significantly alter spontaneous locomotor activity at 3, 10, 30 mg/kg.
Chemical Information
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CAS No. 926493-93-8
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Masse moléculaire 396.52
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Formule C24H32N2O3
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SMILES
C/C=C/C1=CC(OC)=C(C=C1)OCC(CN2CCN(CC2)CC3=CC=CC=C3)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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