2. Membrane Transporter/Ion Channel
  3. Monoamine Transporter
  4. 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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F3288-0031

F3288-0031 Chemical Structure

CAS No. : 926493-93-8

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Description

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[1].

Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration
Mice[1] 30 mg/kg i.p. 8.31 μM 52.2 μM
In Vivo

F3288-0031 (3-50 mg/kg, i.p., once) has an antidepressant-like activity without confounding locomotor effects in C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice (6-8 weeks)[1]
Dosage: 3, 10, 30, 50 mg/kg
Administration: i.p., once
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.
Molecular Weight

396.52

Formula

C24H32N2O3
CAS No.
SMILES

C/C=C/C1=CC(OC)=C(C=C1)OCC(CN2CCN(CC2)CC3=CC=CC=C3)O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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F3288-0031 Related Classifications

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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:

F3288-0031926493-93-8Monoamine TransporterNETNET/SERTdepressive disorderInhibitorinhibitorinhibit

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