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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $60 | In Stock | In Stock | |
| 10 mg | $89 | In Stock | In Stock | |
| 25 mg | $179 | In Stock | In Stock | |
| 50 mg | $288 | In Stock | In Stock | |
| 100 mg | $467 | - | In Stock | |
| 200 mg | $669 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $68 | In Stock | In Stock |
| 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). |
| Synonyms | JNJ 63533054 |
| Molecular Weight | 316.78 |
| Formula | C17H17ClN2O2 |
| Cas No. | 1802326-66-4 |
| Smiles | C[C@H](NC(=O)CNC(=O)c1cccc(Cl)c1)c1ccccc1 |
| Relative Density. | 1.224 g/cm3 (Predicted) |
| Storage | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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