JNJ 63533054
- Product Name
- JNJ 63533054
- CAS No.
- 1802326-66-4
- Chemical Name
- JNJ 63533054
- Synonyms
- CS-2223;JNJ 63533054;JNJ 63533054 ，S6425;JNJ-63533054 (JNJ63533054;JNJ-63533054 >=98% (HPLC);JNJ-63533054, 10 mM in DMSO;(S)-3-Chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide;3-Chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide;Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-;L-tryptophan,blood-brain,oral,CNS,L-phenylalanine,G Protein-Coupled Receptor 139,barrier,JNJ63533054,Inhibitor,GPR139,JNJ-63533054,inhibit
- CBNumber
- CB43110757
- Molecular Formula
- C17H17ClN2O2
- Formula Weight
- 316.78
- MOL File
- 1802326-66-4.mol
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.
N-Bromosuccinimide Price
- Product number
- SML1624
- Product name
- JNJ-63533054
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $94.4
- Updated
- 2025/07/31
- Product number
- SML1624
- Product name
- JNJ-63533054
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $380
- Updated
- 2025/07/31
- Product number
- 23450
- Product name
- JNJ-63533054
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 23450
- Product name
- JNJ-63533054
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 23450
- Product name
- JNJ-63533054
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
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.
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 63533054 Preparation Products And Raw materials
Raw materials
Preparation Products
JNJ 63533054 Suppliers
- Tel
- --
- Fax
- --
- sales@ajchem.in
- Country
- India
- ProdList
- 6100
- Advantage
- 58
View Lastest Price from JNJ 63533054 manufacturers
- Product
- JNJ 63533054 1802326-66-4
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 20kg
- Release date
- 2019-12-23