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NK3R-IN-2

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Catalog No. T210743

NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM against human NK3R. It can penetrate the blood-brain barrier and exhibits excellent NK3R binding affinity in CHO-K1 cells (IC50= 87.31 nM). NK3R-IN-2 effectively suppresses luteinizing hormone (LH) levels and is applicable for research on hormone-related diseases.

NK3R-IN-2

NK3R-IN-2

😃Good
Catalog No. T210743
NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM against human NK3R. It can penetrate the blood-brain barrier and exhibits excellent NK3R binding affinity in CHO-K1 cells (IC50= 87.31 nM). NK3R-IN-2 effectively suppresses luteinizing hormone (LH) levels and is applicable for research on hormone-related diseases.
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Product Introduction

Bioactivity
Description
NK3R-IN-2 is an orally active NK3R inhibitor with an IC50 of 330.50 nM against human NK3R. It can penetrate the blood-brain barrier and exhibits excellent NK3R binding affinity in CHO-K1 cells (IC50= 87.31 nM). NK3R-IN-2 effectively suppresses luteinizing hormone (LH) levels and is applicable for research on hormone-related diseases.
In vitro
NK3R-IN-2 (Compound 22i) (1 μM) demonstrates good metabolic stability in human and rat liver microsomes. At concentrations ranging from 0.3 to 30 μM, NK3R-IN-2 does not significantly inhibit the hERG channel (IC 50 = 31.7 μM), nor does it exhibit notable cardiotoxicity.
In vivo
NK3R-IN-2 (Compound 22i) administered at 5 mg/kg orally in male Sprague-Dawley rats demonstrates excellent blood-brain barrier permeability and low hepatotoxicity. At a dose of 70 mg/kg administered orally, NK3R-IN-2 significantly reduces luteinizing hormone (LH) levels in ovariectomized (OVX) Sprague-Dawley rats.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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