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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- Formel: C17H18Cl2FN3O
- Molecular Weight:370.25
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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nNOS 16 nM (Ki) |
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.
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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Molecular Weight 370.25
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
nNOS-IN-6 Related Classifications
HY-181711 Related Classifications
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