Home GPCR & G Protein GPR agonist JNJ 63533054

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JNJ 63533054 GPR agonist

Cat.No.S6425

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 GPR agonist Chemical Structure

Chemical Structure

Molecular Weight: 316.78

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Quality Control

Batch: S642501 DMSO]63 mg/mL]false]]]false]]]false Purity: 99.73%
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99.73

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (198.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 316.78 Formula

C17H17ClN2O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1802326-66-4 -- Storage of Stock Solutions

Synonyms N/A Smiles CC(C1=CC=CC=C1)NC(=O)CNC(=O)C2=CC(=CC=C2)Cl

Mechanism of Action

Targets/IC50/Ki
human GPR139
(Cell-free assay)
0.024 μM(Ki)
mouse GPR139
(Cell-free assay)
0.054 μM(Ki)
rat GPR13
(Cell-free assay)
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).
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.
References

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