AC-5216
- CAS号:226954-04-7
- 英文名:AC-5216
- 中文名:AC-5216
- CBNumber:CB32448636
- 分子式:C23H23N5O2
- 分子量:401.46
- MOL File:226954-04-7.mol
- 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 :powder
- 颜色 :white to beige
AC-5216性质、用途与生产工艺
- 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
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 -
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).
- 更新日期：2024/11/08
- 产品编号：HY-15527
- 产品名称：Emapunil
- CAS编号：
- 包装：1 mg
- 价格：400元
- 更新日期：2024/11/08
- 产品编号：HY-15527
- 产品名称：Emapunil
- CAS编号：226954-04-7
- 包装：5mg
- 价格：900元
- 公司名称：Novachemistry
- 联系电话：44-20819178-90 02081917890
- 电子邮件：info@novachemistry.com
- 国家：英国
- 产品数：4381
- 优势度：58
- 公司名称：Sinbond Industiral Co., Ltd.
- 联系电话：--
- 电子邮件：cici1124@gmail.com
- 国家：英国
- 产品数：248
- 优势度：50
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
