JNJ 63533054 Chemical Properties

Boiling point:

559.7±45.0 °C(Predicted)

Density 

1.224±0.06 g/cm3(Predicted)

storage temp. 

room temp

solubility 

Soluble in DMSO (up to 35 mg/ml).

form 

powder

pka

12.77±0.46(Predicted)

color 

white to beige

optical activity

[α]/D -89 to -99°, c = 1 in ethanol

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.

JNJ 63533054 Usage And Synthesis

Description

JNJ-63533054 (1802326-66-4) is a potent and selective brain-penetrant GPR139 agonist (EC50=16 nM) an orphan G-protein-coupled receptor expressed in the CNS.1?Tritium-labeled JNJ-63533054 binds to cell membranes expressing GPR139 and can be displaced by putative endogenous ligands.2?Decreases compulsive-like alcohol drinking and hyperalgesia in alcohol-dependent rodents.3?Suppresses morphine intake in a mouse self-administration model.4

Uses

JNJ 63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

Biochem/physiol Actions

JNJ-63533054 is a potent and selective agonist of the orphan receptor hGPR139, a GPCR receptor expressed in the brain in circumventricular regions of the habenula and septum. JNJ-63533054 has an EC50 value of 16 nM, crosses the blood-brain barrier, and is orally available.

storage

Store at RT

References

1) Dvorak?et al.?(2015),?Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor;?ACS Med. Chem. Lett.,?6?1015 2) Liu?et al. (2015),?GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine; Mol. Pharmacol.,?88?911 3) Kononoff?et al.?(2018),?Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-Like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats;?eNeuro,?5?ENEURO 0153-18 2018 4) Wang?et al.?(2019),?Genetic behavioral screen identifies an orphan anti-opioid system; Science,?365?1267

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