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JNJ-31020028

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Catalog No. T1997Cas No. 1094873-14-9
Alias JNJ 31020028

JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22, rat); it exhibits >100-fold selectivity for Y2 versus human Y1/Y4/Y5 receptors.

JNJ-31020028

JNJ-31020028

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Purity: 99.65%
Catalog No. T1997Alias JNJ 31020028Cas No. 1094873-14-9
JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22, rat); it exhibits >100-fold selectivity for Y2 versus human Y1/Y4/Y5 receptors.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$43In StockIn Stock
10 mg$70In StockIn Stock
25 mg$130In StockIn Stock
50 mg$223In StockIn Stock
100 mg$333-In Stock
200 mg$478-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.65%
Color:White
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Product Introduction

JNJ-31020028 AI Summary
JNJ-31020028 exhibits significant bioactivity as a Y2 receptor antagonist, evidenced by its ability to displace [125I]PYY from the human NPY Y2 receptor with an IC50 value of 6.0 nM. This suggests its potential for modulating the neuropeptide Y (NPY) pathway, which is involved in numerous physiological processes, including appetite regulation, stress response, and cardiovascular function. In vivo studies show it has an ED50 of 1.6 mg/kg for NPYY5 receptor occupancy in rat brain, with 90% activity observed at 10 mg/kg. The compound also demonstrates high selectivity for NPYY5, NPYY4, and NPYY1 receptors. However, it shows low metabolic stability, with only 1.7% and 1.4% remaining after 15 minutes in rat and human liver microsomes, respectively. Additionally, JNJ-31020028 exhibits moderate inhibitory activity against MTP with an IC50 value of 710.0 nM. Pharmacokinetic properties include a half-life of 0.83 hours, a Cmax of 4350.0 nM, 100% bioavailability when administered subcutaneously at 10 mg/kg, and 6.0% oral bioavailability in rats. In terms of antiviral activity, JNJ-31020028 shows limited inhibition of SARS-CoV-2 3CL-Pro protease and VERO-6 cell cytotoxicity, with 4.52% inhibition at 20 µM and 0.31% at 10 µM after 48 hours, respectively..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22, rat); it exhibits >100-fold selectivity for Y2 versus human Y1/Y4/Y5 receptors.
Targets&IC50
Y2 receptor (human):8.07(pIC50), Y2 receptor (rat):8.22(pIC50)
SynonymsJNJ 31020028
Chemical Properties
Molecular Weight565.68
FormulaC34H36FN5O2
Cas No.1094873-14-9
SmilesCCN(CC)C(=O)C(N1CCN(CC1)c1ccc(NC(=O)c2ccccc2-c2cccnc2)cc1F)c1ccccc1
Relative Density.1.228 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 5.66 mg/mL (10.01 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.77 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7678 mL8.8389 mL17.6778 mL88.3892 mL
5 mM0.3536 mL1.7678 mL3.5356 mL17.6778 mL
10 mM0.1768 mL0.8839 mL1.7678 mL8.8389 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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