3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
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- CAS号:
- 1802326-66-4
- 英文名:
- JNJ 63533054
- 英文别名:
- CS-2223;JNJ 63533054;JNJ-63533054 (JNJ63533054;JNJ-63533054 >=98% (HPLC);(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
- 中文名:
- 3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
- 中文别名:
- 化合物JNJ63533054;JNJ-63533054游离态;JNJ 63533054,GPR139激动剂;(S)-3-氯-N-(2-氧代-2-((1-苯基乙基)氨基)乙基)苯甲酰胺;3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
- CBNumber:
- CB43110757
- 分子式:
- C17H17ClN2O2
- 分子量:
- 316.78
- MOL File:
- 1802326-66-4.mol
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3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺化学性质
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沸点:
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559.7±45.0 °C(Predicted)
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密度:
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1.224±0.06 g/cm3(Predicted)
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储存条件:
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room temp
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溶解度:
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Soluble in DMSO (up to 35 mg/ml).
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酸度系数(pKa):
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12.77±0.46(Predicted)
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形态:
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powder
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颜色:
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white to beige
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旋光性 (optical activity):
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[α]/D -89 to -99°, c = 1 in ethanol
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稳定性:
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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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3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺性质、用途与生产工艺
JNJ 63533054是一种有效的、选择性GPR139激动剂，在钙动员和GTPγS结合实验中特异性地激活人源GPR139，EC50分别为16 ± 6 nM和17 ± 4 nM。
| Target | Value |
human GPR139
(Cell-free assay)
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0.024 μM(Ki)
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mouse GPR139
(Cell-free assay)
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0.054 μM(Ki)
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rat GPR13
(Cell-free assay)
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0.075 μM(Ki)
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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).
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.
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Animal Model:
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Male Sprague-Dawley rats (350-450 g)
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Dosage:
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3 mg/kg, 10 mg/kg, and 30 mg/kg
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Administration:
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Oral administration; once
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Result:
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Induced a dose-dependent reduction in locomotor activity in the first hour.
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3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-19838 | JNJ-63533054 | | 1 mg | 295元 |
| 2024/01/25 | HY-19838 | 3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
JNJ-63533054 | 1802326-66-4 | 5mg | 650元 |
3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
生产厂家
1802326-66-4, 3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺 相关搜索:
- 合成有机化合物配体
- 化工试剂
- JNJ 63533054,GPR139激动剂
- (S)-3-氯-N-(2-氧代-2-((1-苯基乙基)氨基)乙基)苯甲酰胺
- JNJ-63533054游离态
- 化合物JNJ63533054
- 3-氯-N-[2-氧代-2-[[(1S)-1-苯基乙基]氨基]乙基]苯甲酰胺
- 1802326-66-4
- L-tryptophan,blood-brain,oral,CNS,L-phenylalanine,G Protein-Coupled Receptor 139,barrier,JNJ63533054,Inhibitor,GPR139,JNJ-63533054,inhibit
- (S)-3-Chloro-N-(2-oxo-2-((1-phenylethyl)amino)ethyl)benzamide
- JNJ-63533054 >=98% (HPLC)
- Benzamide, 3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-
- JNJ-63533054 (JNJ63533054
- CS-2223
- 3-Chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]benzamide
- JNJ 63533054