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JNJ-63533054

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Catalog No. T3119Cas No. 1802326-66-4
Alias JNJ 63533054

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

JNJ-63533054

JNJ-63533054

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Purity: 99.88%
Catalog No. T3119Alias JNJ 63533054Cas No. 1802326-66-4
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$60In StockIn Stock
10 mg$89In StockIn Stock
25 mg$179In StockIn Stock
50 mg$288In StockIn Stock
100 mg$467-In Stock
200 mg$669-In Stock
1 mL x 10 mM (in DMSO)$68In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.88%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
Targets&IC50
GPR139:16 Nm(EC50)
In vitro
JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. JNJ-63533054 is found to be clean of any cross reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters as well as our own internal whole cell lead generation biology selectivity panel.
In vivo
JNJ-63533054 is found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat. JNJ-63533054 exhibits good stability in both human and rat microsomes and high solubility in aqueous media, and no DDI potential was found. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM).
SynonymsJNJ 63533054
Chemical Properties
Molecular Weight316.78
FormulaC17H17ClN2O2
Cas No.1802326-66-4
SmilesC[C@H](NC(=O)CNC(=O)c1cccc(Cl)c1)c1ccccc1
Relative Density.1.224 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: 45 mg/mL (142.05 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.31 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 mM3.1568 mL15.7838 mL31.5676 mL157.8382 mL
5 mM0.6314 mL3.1568 mL6.3135 mL31.5676 mL
10 mM0.3157 mL1.5784 mL3.1568 mL15.7838 mL
20 mM0.1578 mL0.7892 mL1.5784 mL7.8919 mL
50 mM0.0631 mL0.3157 mL0.6314 mL3.1568 mL
100 mM0.0316 mL0.1578 mL0.3157 mL1.5784 mL

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In Vivo Formulation Calculator (Clear solution)

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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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