JNJ 63533054

Catalog No.S6425

For research use only.

JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.

JNJ 63533054 Chemical Structure

CAS No. 1802326-66-4

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Biological Activity

Description JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
Targets
human GPR139 [1]
(Cell-free assay)
mouse GPR139 [1]
(Cell-free assay)
rat GPR13 [1]
(Cell-free assay)
0.024 μM(Ki) 0.054 μM(Ki) 0.075 μM(Ki)
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 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM)[1].

In vivo

The small-molecule JNJ-63533054 is found to be devoid of any cross-reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters, and it displays suitable pharmacokinetic properties for in vivo studies. JNJ-63533054 crosses the rat blood-brain barrier after oral administration and achieves exposure in the micromolar range. JNJ-63533054 administration decreases spontaneous locomotor activity in rats[1].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: male Sprague-Dawley rats (350-450 g)
  • Dosages: 3, 10, and 30 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

DMSO 63 mg/mL
(198.87 mM)


Chemical Information

Molecular Weight 316.78
Formula

C17H17ClN2O2

CAS No. 1802326-66-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC=CC=C1)NC(=O)CNC(=O)C2=CC(=CC=C2)Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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