Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-
JNJ 63533054
CAS: 1802326-66-4
Molecular Formula: C17H17ClN2O2
Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]- - Names and Identifiers
Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]- - Physico-chemical Properties
| Molecular Formula | C17H17ClN2O2 |
| Molar Mass | 316.78 |
| Solubility | DMSO : 50 mg/mL (157.84 mM);H2O : < 0.1 mg/mL (insoluble) |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | room temp |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
| In vitro study | JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC 50 of 16 nM) and GTPγS binding (EC 50 of 17 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC 50 of 63 nM, mouse EC 50 of 28 nM). In a saturation study for human GPR139, a single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (K d of 10 nM). The B max value is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded K d values within the same range (32 nM and 23 nM, respectively; B max = 8.5 pmol/mg of protein and 6.2 pmol/mg of protein, respectively). |
| In vivo study | JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour. 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 C max is 317 ng/mL (~1 μM), the t 1/2 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. Animal Model: Male Sprague-Dawley rats (350-450 g) 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. |
Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.157 ml | 15.784 ml | 31.567 ml |
| 5 mM | 0.631 ml | 3.157 ml | 6.313 ml |
| 10 mM | 0.316 ml | 1.578 ml | 3.157 ml |
| 5 mM | 0.063 ml | 0.316 ml | 0.631 ml |
Last Update：2024-01-02 23:10:35
Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]- - Reference Information
| biological activity | JNJ 63533054 is an effective and selective GPR139 agonist, which specifically activates human GPR139 in calcium mobilization and GTP γS binding experiments, with EC50 of 16±6 nM and 17±4 nM respectively. |
| target | TargetValue human GPR139 (Cell-free say) 0.024 μM(Ki) mouse GPR139 (Cell-free say) 0.054 μM(Ki) rat GPR13 (Cell-free say) 0.075 μM(Ki) |
| Target | Value |
| human GPR139 (Cell-free assay) | 0.024 μM(Ki) |
| mouse GPR139 (Cell-free assay) | 0.054 μM(Ki) |
| rat GPR13 (Cell-free assay) | 0.075 μM(Ki) |
| in vitro study | JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC 50 of 16 nM) and GTP γ S binding (EC 50 of 17 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC 50 of 63 nM, mouse EC 50 of 28 nM). In a saturation study for human GPR139, A single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (K d of 10 nM). The B max value is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded K d values in the same range (32 nM and 23 nM, respectively; B max = 8.5 pmol/mg of protein and 6.2 pmol/mg of protein, respectively). |
| in vivo studies | JNJ-63533054 (3-30 mg/kg; oral administration; once; SD rats) treatment induces a dose-dependent reduction in locomotor activity in the first hour. 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 C max is 317 ng/ml (~ 1 μ m), the t 1/2 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. Animal model: male Sprague-Dawley rat (350-450g) 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. |
| Animal Model: | Male Sprague-Dawley rats (350-450 g) |
| 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. |
Last Update：2024-04-09 22:09:11
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Spot supply
Product Name: JNJ 63533054 Visit Supplier Webpage Request for quotationCAS: 1802326-66-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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