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.
For research use only. We do not sell to patients.
- Formula: C18H14ClFN6OS
- Molecular Weight:416.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NK3R |
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.
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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Molecular Weight 416.86
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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