JNJ 63533054

Catalog No.S6425

JNJ 63533054 Chemical Structure

Molecular Weight(MW): 316.78

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.

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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

Animal Research:

[1]

- Collapse
  • Animal Models: male Sprague-Dawley rats (350-450 g)
  • Formulation: 0.5% hydroxypropyl methylcellulose in suspension
  • Dosages: 3, 10, and 30 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 63 mg/mL (198.87 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 316.78
Formula

C17H17ClN2O2

CAS No. 1802326-66-4
Storage powder
in solvent
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID