2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. NK3R antagonist-1

NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes.

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NK3R antagonist-1

NK3R antagonist-1 Chemical Structure

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NK3R antagonist-1 Related Antibodies

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Description

NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes[1].

IC50 & Target[1]

NK3R

53.61 nM (IC50)

In Vitro

NK3R antagonist-1 (Compound 23i(R)) (0.30-30 μM) inhibits hERG potassium channels in CHO-K1 cells, with an IC50 value of 34.5 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NK3R antagonist-1 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC0-last CL Vz T1/2 Tmax Bioavailability
Rat[1] 1 mg/kg i.v. 3154 ng/mL 3487 ng·h/mL 286 mL/h/kg 504 mL/kg 1.2 h / /
Rat[1] 5 mg/kg i.g. 3920 ng/mL 28867 ng·h/mL / / 2.16 h 0.25 h 165 %
In Vivo

NK3R antagonist-1 (Compound 23i(R)) (120 mg/kg; i.g.; single dose) significantly suppresses plasma luteinizing hormone levels in ovariectomized rats, with inhibitory activity detectable as early as 45 min post-dose[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 8-12 weeks old, ovariectomized)[1]
Dosage: 120 mg/kg
Administration: i.g.; single dose
Result: Significantly reduced plasma luteinizing hormone (LH) levels, with inhibitory effect evident at 45 min post-dose, and statistically significant differences relative to vehicle control observed at both 45 and 90 min post-dose.
Molecular Weight

395.45

Formula

C20H18FN5OS
SMILES

CC1=NSC(C2=NC(C#CC)=C([C@H]3C)N2CCN3C(C4=CC=C(F)C=C4)=O)=N1
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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NK3R antagonist-1 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 antagonist-1Neurokinin ReceptorNK receptorTachykinin receptorhuman NK3RHEK293T cellsCHO-K1 cell membrane preparationsovariectomized rat modelsmenopausal hot flashesblood-brain barrierluteinizing hormonehERG potassium channelsCHO-K1 cellsneurokinin-3 receptorInhibitorinhibitorinhibit

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