nNOS-PDZ-IN-1
nNOS-PDZ-IN-1 is an orally active, blood-brain barrier-penetrant inhibitor of neuronal nitric oxide synthase-PDZ domain (nNOS-PDZ), with an IC50 of 0.76 μM and a KD of 0.55 μM. nNOS-PDZ-IN-1 binds to the nNOS-PDZ domain, occupies its binding site and disrupts its interaction with the serotonin transporter. nNOS-PDZ-IN-1 exhibits antidepressant activity without addiction potential or movement-related side effects. nNOS-PDZ-IN-1 can be used in research related to major depressive disorder.
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- Formule: C15H11F2NO3S
- Masse moléculaire:323.31
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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
nNOS-PDZ-IN-1 (Compound N24) (30 min) shows no inhibitory activity against purified recombinant human APBA1-1, APBA3-1, ZO1-2 and LNX2-2 PDZ domain proteins, only exhibits weak activity against LNX1-2, and displays high selectivity for the nNOS-PDZ domain in FP assays[1].
nNOS-PDZ-IN-1 (2.5-40 μM; 2 h) dose-dependently disrupts the interaction between nNOS and SERT in 293T cells co-expressing full-length human nNOS and SERT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
nNOS-PDZ-IN-1 (10-30 mg/kg; p.o.; single administration) exerts rapid and dose-dependent antidepressant effects in mice subjected to the chronic unpredictable mild stress (CUMS) model[1].
Oral administration of nNOS-PDZ-IN-1 at 250 mg/kg once daily for 14 days causes no obvious toxicity or organ damage in healthy C57BL/6J mice[1].
nNOS-PDZ-IN-1 (30 mg/kg; p.o.) does not induce conditioned place preference when administered at an oral dose of 30 mg/kg, indicating that it has no significant addictive potential in healthy male C57BL/6J mice[1].
nNOS-PDZ-IN-1 (30 mg/kg; p.o.; single administration) does not impair motor coordination or balance in healthy C57BL/6J mice at an oral dose of 30 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (6-8 weeks old, ~20 g, chronic corticosterone-induced depression model)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Increased total distance traveled in the open field test at both 10 mg/kg and 30 mg/kg, with a larger increase at 30 mg/kg.
Reduced immobility time in the tail suspension test at both 10 mg/kg and 30 mg/kg, with a larger reduction at 30 mg/kg.
Reduced immobility time in the forced swim test at both 10 mg/kg and 30 mg/kg, with a larger reduction at 30 mg/kg.
Produced statistically significant effects at both doses.
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Animal Model:C57BL/6J (6-8 weeks old, ~20 g, chronic unpredictable mild stress model)[1]
-
Dosage:10 mg/kg; 30 mg/kg
-
Administration:p.o.; single dose
-
Result:Increased total distance traveled in the open field test at both 10 mg/kg and 30 mg/kg, with a larger increase at 30 mg/kg.
Reduced immobility time in the tail suspension test at both 10 mg/kg and 30 mg/kg, with a larger reduction at 30 mg/kg.
Reduced the nNOS-SERT complex level in the dorsal raphe nucleus at 30 mg/kg.
Produced statistically significant effects at both doses.
Chemical Information
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Masse moléculaire 323.31
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Formule C15H11F2NO3S
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SMILES
FC1=CC(CC2=C(C=C(C=C2)C)F)=CC3=C1OS(N=C3)(=O)=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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