2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. 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.

NK3R-IN-2 Chemical Structure

NK3R-IN-2 Chemical Structure

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NK3R-IN-2 Related Antibodies

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Description

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[1].

IC50 & Target

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.

NK3R-IN-2 Related Antibodies
In Vivo

NK3R-IN-2 (Compoud 22i) (5 mg/kg, i.g.; single dose) exhibits excellent blood-brain barrier permeability and low liver toxicity in the male Sprague-Dawley rats[1].
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.

Animal Model: Male Sprague-Dawley rats (6-8 weeks, 180-220g)[1]
Dosage: 5 mg/kg
Administration: Oral gavage (i.g.); once at 1, 4 and 10 hours
Result: Was slightly higher than the level of ESN364 (HY-19632) in the brain.
Had a low concentration in the liver.
Animal Model: Ovariectomized (OVX) Sprague-Dawley rats (6-8 weeks, 180-220g)[1]
Dosage: 70 mg/kg
Administration: Oral gavage (i.g.); single dose
Result: Significantly reduced plasma LH concentration.
Molecular Weight

416.86

Formula

C18H14ClFN6OS
SMILES

N#CC1=C2C(C)N(C(C3=CC=C(Cl)C(F)=C3)=O)CCN2C(C4=NC(C)=NS4)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NK3R-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NK3R-IN-2Neurokinin ReceptorNK receptorTachykinin receptorNK3RAntagonistEndocrinologyluteinizing hormoneInhibitorinhibitorinhibit

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