返回ChemicalBook首页>CAS数据库列表>226954-04-7

226954-04-7

中文名称 N/A
英文名称 AC-5216
CAS 226954-04-7
分子式 C23H23N5O2
分子量 401.46
MOL 文件 226954-04-7.mol
更新日期 2024/08/07 17:48:13
226954-04-7 结构式 226954-04-7 结构式

基本信息

中文别名
EMAPUNIL游离
EMAPUNIL游离态
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
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
英文别名
CS-2606
AC-5216
XBD-173
EMapunil
Emapunil(AC-5216)
AC 5216 (Emapunil)
XBD173 >=98% (HPLC)
AC-5216
XBD-173
EMAPUNIL
AC5216
AC 5216
N-Benzyl-N-ethyl-2-(7-Methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetaMide
N-Ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-9H-purine-9-acetamide
所属类别
生物化工:激动剂抑制剂

物理化学性质

储存条件2-8°C
溶解度DMF: 30 mg/mL; DMF:PBS (pH 7.2) (1:20): 0.05 mg/mL; DMSO: 5 mg/mL
形态粉末
颜色白色至米色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302

常见问题列表

生物活性
Emapunil (AC-5216, 18 kiloDalton Translocator Protein, XBD173)是一种新型的 mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) 配体。Emapunil(AC-5216) 对大鼠全脑制备的 MBRs 具有高亲和力,Ki值为0.297 nM,在大鼠神经胶质瘤细胞和人神经胶质瘤细胞上的IC50值分别为 3.04 nM和 2.73 nM。
靶点
TargetValue
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
体内研究

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).
"226954-04-7" 相关产品信息