Other grades of this product :
| JNJ 63533054 Basic information |
| Product Name: | JNJ 63533054 | | Synonyms: | JNJ 63533054;3-Chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide;CS-2223;JNJ-63533054 (JNJ63533054;Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-;JNJ-63533054 >=98% (HPLC);(S)-3-Chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide | | CAS: | 1802326-66-4 | | MF: | C17H17ClN2O2 | | MW: | 316.78 | | EINECS: | | Product Categories: | | Mol File: | 1802326-66-4.mol |
| JNJ 63533054 Chemical Properties |
| storage temp. | room temp | | solubility | Soluble in DMSO (up to 35 mg/ml). | | form | powder | | 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. | | 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 |
| JNJ 63533054 Preparation Products And Raw materials |
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