中文名 | JNJ 63533054 |
英文名 | JNJ 63533054 |
别名 | 化合物JNJ63533054 JNJ-63533054游离态 3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺 |
英文别名 | CS-2223 JNJ 63533054 JNJ-63533054 (JNJ63533054 3-Chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]- |
CAS | 1802326-66-4 |
化学式 | C17H17ClN2O2 |
分子量 | 316.78 |
溶解度 | 溶于DMSO (高达35 mg/ml)。 |
存储条件 | room temp |
稳定性 | 从提供的购买之日起稳定2年。在DMSO中的溶液可以在-20 ° 储存长达2个月。 |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | 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). |
体内研究 | 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. |
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 |
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