2. GPCR/G Protein Neuronal Signaling
  3. GPR139
  4. JNJ-63533054

JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).

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JNJ-63533054 Chemical Structure

JNJ-63533054 Chemical Structure

CAS No. : 1802326-66-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

JNJ-63533054 Related Antibodies

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Description

JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB)[1][2].

IC50 & Target

EC50: 16 nM (Human GPR139), 63 nM (Rat GPR139) and 28 nM (Mouse GPR139)[1]
In Vitro

JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 of 16 nM) and GTPγS binding (EC50 of 17 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 of 63 nM, mouse EC50 of 28 nM)[1].
In a saturation study for human GPR139, a single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (Kd of 10 nM). The Bmax value is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded Kd values within the same range (32 nM and 23 nM, respectively; Bmax = 8.5 pmol/mg of protein and 6.2 pmol/mg of protein, respectively)[1].

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

JNJ-63533054 Related Antibodies
In Vivo

JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour[1].
The pharmacokinetics of JNJ-63533054 (Compound 7c; 1 mg/kg iv; 5 mg/kg po) in rat is examined. The IV clearance is 53 mL/min/kg, the Cmax is 317 ng/mL (~1 μM), the t1/2 is 2.5 hours, and JNJ-63533054 is able to cross the blood-brain barrier (BBB) with a brain to plasma ratio (b/p) of 1.2[2].

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

Animal Model: Male Sprague-Dawley rats (350-450 g)[1]
Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration: Oral administration; once
Result: Induced a dose-dependent reduction in locomotor activity in the first hour.
Molecular Weight

316.78

Formula

C17H17ClN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC(N[C@H](C1=CC=CC=C1)C)=O)C2=CC=CC(Cl)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (157.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1568 mL 15.7838 mL 31.5676 mL
5 mM 0.6314 mL 3.1568 mL 6.3135 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1568 mL 15.7838 mL 31.5676 mL 78.9191 mL
5 mM 0.6314 mL 3.1568 mL 6.3135 mL 15.7838 mL
10 mM 0.3157 mL 1.5784 mL 3.1568 mL 7.8919 mL
15 mM 0.2105 mL 1.0523 mL 2.1045 mL 5.2613 mL
20 mM 0.1578 mL 0.7892 mL 1.5784 mL 3.9460 mL
25 mM 0.1263 mL 0.6314 mL 1.2627 mL 3.1568 mL
30 mM 0.1052 mL 0.5261 mL 1.0523 mL 2.6306 mL
40 mM 0.0789 mL 0.3946 mL 0.7892 mL 1.9730 mL
50 mM 0.0631 mL 0.3157 mL 0.6314 mL 1.5784 mL
60 mM 0.0526 mL 0.2631 mL 0.5261 mL 1.3153 mL
80 mM 0.0395 mL 0.1973 mL 0.3946 mL 0.9865 mL
100 mM 0.0316 mL 0.1578 mL 0.3157 mL 0.7892 mL
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JNJ-63533054 Related Classifications

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:

JNJ-635330541802326-66-4JNJ63533054JNJ 63533054GPR139G Protein-Coupled Receptor 139CNSblood-brainbarrieroralL-tryptophanL-phenylalanineInhibitorinhibitorinhibit

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