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

JNJ-63533054 

Cat. No.: HY-19838 Purity: 99.94%
Handling Instructions

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).

For research use only. We do not sell to patients.

JNJ-63533054 Chemical Structure

JNJ-63533054 Chemical Structure

CAS No. : 1802326-66-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
5 mg USD 78 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 828 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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.

1802326-66-4

SMILES

O=C(NCC(N[[email protected]](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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (157.84 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.3157 mL 1.5784 mL 3.1568 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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Product Name:
JNJ-63533054
Cat. No.:
HY-19838
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