AC-5216
| 中文名称 | AC-5216 |
|---|---|
| 中文同义词 | EMAPUNIL游离态;EMAPUNIL游离;N-苄基-N-乙基-2-(7-甲基-8-氧代-2-苯基-7,8-二氢-9H-嘌呤-9-基)乙酰胺;N-乙基-7,8-二氢-7-甲基-8-氧代-2-苯基-N-(苯基甲基)-9H-嘌呤-9-乙酰胺;依马普尼;AC 5216,TSPO配体 |
| 英文名称 | AC-5216 |
| 英文同义词 | EMapunil;XBD-173;N-Benzyl-N-ethyl-2-(7-Methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetaMide;9H-Purine-9-acetaMide,N-ethyl-7,8-dihydro-7-Methyl-8-oxo-2-phenyl-N-(phenylMethyl)-;AC 5216 (Emapunil);N-Ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-9H-purine-9-acetamide;Emapunil(AC-5216);AC-5216 |
| CAS号 | 226954-04-7 |
| 分子式 | C23H23N5O2 |
| 分子量 | 401.46 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;活性分子;Inhibitors |
| Mol文件 | 226954-04-7.mol |
| 结构式 |  |
AC-5216 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | DMF：30mg/mL； DMF:PBS (pH 7.2) (1:20)：0.05 mg/mL；二甲基亚砜：5mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| Target | Value |
|
mMBR(Brain)
(Cell-free assay) | 0.297 nM(Ki) |
|
MBR
(human glioma cells-based assay) | 2.73 nM |
|
MBR
(rat glioma cells-based assay) | 3.04 nM |
Emapunil (AC-5216, 0.1-3, 0.003-0.01 and 0.01-0.3 mg/kg, p.o.) produces anti-anxiety effects in the Vogel-type conflict test in rats, and in the light/dark box and social interaction tests in mice.
Emapunil (AC-5216, 3-30 mg/kg, p.o.) reduces the immobility time, and this effect was blocked by PK11195.
Emapunil (AC-5216, 1-100 mg/kg, p.o.) produces no distinct change in the rat electroencephalogram.
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) causes significant suppression of the enhanced anxiety and contextual fear induced in post-TDS rats.
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) alleviates the enhanced anxiety and fear response in a time-dependent sensitization (TDS) procedure, a rat PTSD animal model.
Emapunil (AC-5216, 0.3 and 1 mg/kg, i.g.) reverses the increased plasma glucose (PG) and decreased insulin (INS) in HFD-STZ rats.
| Animal Model: | Rats. |
| Dosage: | 0.1-3 mg/kg. |
| Administration: | P.O.. |
| Result: |
Significantly increased the number of shocks that rats received.
Significantly increased the time spent in the light compartment but only slightly increased that time at 0.03 mg/kg, p.o. (P<0.1). |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-15527 | Emapunil | 1 mg | 400元 | |
| 2024/08/19 | HY-15527 | Emapunil | 226954-04-7 | 5mg | 900元 |