nNOS-IN-6
nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma.
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- Formule: C17H18Cl2FN3O
- Masse moléculaire:370.25
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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
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Activité biologique
Description
IC50 & Target
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nNOS 16 nM (Ki) |
In Vitro
nNOS-IN-6 (compound 16) potently inhibits human neuronal nitric oxide synthase (hnNOS) with a Ki of 16 nM, and exhibits approximately 1800-fold selectivity over human endothelial nitric oxide synthase (heNOS) and approximately 2900-fold selectivity over human inducible nitric oxide synthase (hiNOS)[1].
nNOS-IN-6 (200 μM; 17 h) exhibits high effective permeability (13.04×10-6 cm/s) in the PAMPA-BBB assay, demonstrating potent central nervous system penetration potential[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (male)[1]
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Dosage:3 mg/kg (i.v.);
10 mg/kg (p.o.) -
Administration:i.v.; single dose; p.o.; single dose
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Result:Exhibited initial plasma concentration (C0) of 654.08 ng/mL at 0.083 h, AUClast of 654.03 h·ng/mL, terminal half-life (t1/2) of 2.49 h, systemic clearance of 74.6 mL/min/kg, steady-state volume of distribution (Vss) of 16.08 L/kg after intravenous administration.
Reached plasma Cmax of 86.51 ng/mL at 1.0 h, AUClast of 356.54 h·ng/mL, t1/2 of 7.96 h, Vss of 222.69 L/kg, oral bioavailability of 16.4% after oral administration.
Achieved brain Cmax of 172.0 ng/g at 12.0 h, brain-Kp (AUClast) of 24.0 after oral administration.
Chemical Information
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Masse moléculaire 370.25
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Formule C17H18Cl2FN3O
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SMILES
CC1=C2C=C(C(C3=CC=C(C(CN)=C3)O)=CC2=NC(N)=C1)F.Cl.Cl
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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)
nNOS-IN-6 Related Classifications
HY-181711 Related Classifications
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