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226954-04-7

中文名稱 N/A
英文名稱 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 2024/11/11 15:36:59
226954-04-7 結(jié)構(gòu)式 226954-04-7 結(jié)構(gòu)式

基本信息

中文別名
EMAPUNIL游離
EMAPUNIL游離態(tài)
N-乙基-7,8-二氫-7-甲基-8-氧代-2-苯基-N-(苯基甲基)-9H-嘌呤-9-乙酰胺
N-芐基-N-乙基-2-(7-甲基-8-氧代-2-苯基-7,8-二氫-9H-嘌呤-9-基)乙酰胺
英文別名
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
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

儲存條件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
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302

常見問題列表

生物活性
Emapunil (AC-5216, 18 kiloDalton Translocator Protein, XBD173)是一種新型的 mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) 配體。Emapunil(AC-5216) 對大鼠全腦制備的 MBRs 具有高親和力,Ki值為0.297 nM,在大鼠神經(jīng)膠質(zhì)瘤細胞和人神經(jīng)膠質(zhì)瘤細胞上的IC50值分別為 3.04 nM和 2.73 nM。
靶點
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
體內(nèi)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).
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