JNJ 63533054 Property

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.

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

JNJ 63533054 Chemical Properties,Usage,Production

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