| 中文名称: | JNJ-63533054 促销 | ||||
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| 英文名称: | JNJ-63533054 | ||||
| 别名: | 3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺 (S)-3-Chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide | ||||
| CAS No: | 1802326-66-4 | 分子式: | C17H17ClN2O2 | 分子量: | 316.78 |
| CAS No: | 1802326-66-4 | ||||
| 分子式: | C17H17ClN2O2 | ||||
| 分子量: | 316.78 | ||||
基本信息
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产品编号： |
J10001 |
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产品名称： |
JNJ-63533054 |
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CAS: |
1802326-66-4 |
储存条件 |
粉末 |
室温 |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
316.78 |
-20℃ |
1个月 |
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化学名： |
(S)-3-Chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide |
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Solubility (25°C)： |
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体外:
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DMSO |
63mg/mL (198.87mM) |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.1568mL |
15.7838mL |
31.5676mL |
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5mM |
0.6314mL |
3.1568mL |
6.3135mL |
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10mM |
0.3157mL |
1.5784mL |
3.1568mL |
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50mM |
0.0631mL |
0.3157mL |
0.6314mL |
生物活性
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产品描述 |
一种强效的选择性的HGPR139激动剂。 |
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靶点 |
human GPR139 |
mouse GPR139 |
rat GPR13 |
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0.024μM(Ki) |
0.054μM(Ki) |
0.075μM(Ki) |
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体外研究 |
JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 of 16nM) and GTPγS binding (EC50 of 17nM) assays.JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 of 63nM,mouse EC50 of 28nM).In a saturation study for human GPR139,a single population of high-affinity binding sites for [3H] JNJ-63533054 is observed (Kd of 10nM).The Bmax value is 26 pmol/mg of protein. Saturation studies for the rat GPR139 and mouse GPR139 yielded Kd values within the same range (32nM and 23nM,respectively;Bmax=8.5 pmol/mg of protein and 6.2 pmol/mg of protein,respectively). |
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体内研究 |
JNJ-63533054 (3-30mg/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;1mg/kg iv;5mg/kg po) in rat is examined.The IV clearance is 53mL/min/kg,the Cmax is 317ng/mL (~1μM),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. |
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Animal Model: |
Male Sprague-Dawley rats (350-450g) |
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Dosage: |
3mg/kg,10mg/kg,and 30mg/kg |
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Administration: |
Oral administration;once |
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Result: |
Induced a dose-dependent reduction in locomotor activity in the first hour. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
