NK3R-IN-2
NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM for human NK3R. NK3R-IN-2 can pass through the blood-brain barrier. NK3R-IN-2 has excellent NK3R binding affinity (IC50 = 87.31 nM) in CHO-K1 cells. NK3R-IN-2 effectively inhibits the level of luteinizing hormone (LH). NK3R-IN-2 can be used for research on hormone related conditions.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C18H14ClFN6OS
- Peso molecular:416.86
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
NK3R |
In Vitro
NK3R-IN-2 (Compoud 22i) (1 μM) shows good metabolic stability in human and rat liver microsomes[1].
NK3R-IN-2 (0.3-30 μM) has no significant inhibition on hERG channel (IC50 = 31.7 μM) and no significant cardiac toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
NK3R-IN-2 (70 mg/kg; i.g.; single dose) significantly inhibits luteinizing hormone (LH) levels in Ovariectomized (OVX) Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (6-8 weeks, 180-220g)[1]
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Dosage:5 mg/kg
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Administration:Oral gavage (i.g.); once at 1, 4 and 10 hours
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Result:Was slightly higher than the level of ESN364 (HY-19632) in the brain.
Had a low concentration in the liver.
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Animal Model:Ovariectomized (OVX) Sprague-Dawley rats (6-8 weeks, 180-220g)[1]
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Dosage:70 mg/kg
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Administration:Oral gavage (i.g.); single dose
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Result:Significantly reduced plasma LH concentration.
Chemical Information
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Peso molecular 416.86
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Fòrmula C18H14ClFN6OS
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SMILES
N#CC1=C2C(C)N(C(C3=CC=C(Cl)C(F)=C3)=O)CCN2C(C4=NC(C)=NS4)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NK3R-IN-2 Related Classifications
HY-176546 Related Classifications
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