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JNJ-63533054 | GPR139 agonist, suppresses morphine intake

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

References/Citations
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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Catalog#  10-3880-0005

$70.00
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CAS:
180232666-4
Catalog Number:
10-3880
Activity:
GPR139 agonist, suppresses morphine intake
Chemical Name:
(S)-3-Chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl) benzamide
Molecular Weight:
316.78
Molecular Formula:
C17H17ClN2O2
Solubility:
Soluble in DMSO (up to 35 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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