Basic information Safety Supplier Related

JNJ 63533054

Basic information Safety Supplier Related

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
  • L-tryptophan,blood-brain,oral,CNS,L-phenylalanine,G Protein-Coupled Receptor 139,barrier,JNJ63533054,Inhibitor,GPR139,JNJ-63533054,inhibit
CAS:
1802326-66-4
MF:
C17H17ClN2O2
MW:
316.78
Mol File:
1802326-66-4.mol
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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.
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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.

in vivo

JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour[1].
? The pharmacokinetics of JNJ-63533054 (Compound 7c; 1 mg/kg iv; 5 mg/kg po) in rat is examined. The IV clearance is 53 mL/min/kg,? the Cmax is 317 ng/mL (~1 μM), the t1/2 is 2.5 hours,? and JNJ-63533054 is able to cross the blood-brain barrier (BBB) with a brain to plasma ratio (b/p) of 1.2[2].

Animal Model:Male Sprague-Dawley rats (350-450 g)[1]
Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:Oral administration; once
Result:Induced a dose-dependent reduction in locomotor activity in the first hour.

storage

Store at RT

References

[1] CURT A. DVORAK*. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor[J]. ACS Medicinal Chemistry Letters, 2015, 6 9: 1015-1018. DOI:10.1021/acsmedchemlett.5b00247
[2] CHANGLU LIU. GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.[J]. Molecular Pharmacology, 2015, 88 5: 911-925. DOI:10.1124/mol.115.100412
[3] JENNI KONONOFF. Systemic and Intra-Habenular Activation of the Orphan G Protein-Coupled Receptor GPR139 Decreases Compulsive-Like Alcohol Drinking and Hyperalgesia in Alcohol-Dependent Rats.[J]. eNeuro, 2018. DOI:10.1523/eneuro.0153-18.2018
[4] DANDAN WANG. Genetic behavioral screen identifies an orphan anti-opioid system[J]. Science, 2019, 365 6459. DOI:10.1126/science.aau2078

JNJ 63533054Supplier

Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
Tel
025-66113011 17798518460
Email
cfzhang@aikonchem.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Email
isunpharm@qq.com
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Email
info@adooq.cn
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Email
sales@shjiyipharmatech.com
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