Home GPCR & G Protein GPR agonist JNJ 63533054 For research use only.

JNJ 63533054

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

JNJ 63533054 Chemical Structure

CAS: 1802326-66-4

Purity & Quality Control

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

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

Chemical Information & Solubility

Molecular Weight 316.78 Formula

C17H17ClN2O2
CAS No. 1802326-66-4 SDF --
Smiles CC(C1=CC=CC=C1)NC(=O)CNC(=O)C2=CC(=CC=C2)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 63 mg/mL ( (198.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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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.

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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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