您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Emapunil
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Emapunil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Emapunil图片
CAS NO:226954-04-7
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 401.46
Formula C23H23N5O2
CAS No. 226954-04-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM in DMSO
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) O=C(N(CC)CC1=CC=CC=C1)CN2C(N(C)C3=CN=C(C4=CC=CC=C4)N=C23)=O
Synonyms XBD-173; XBD 173 XBD173; Emapunil; AC-5216; AC 5216; AC5216
实验参考方法
In Vitro

In vitro activity: Emapunil (formerly known as AC-5216 or XBD-173) is an antianxiolytic drug that also has neuroprotective activities. It acts as a potent and selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO. TSPO is a five transmembrane domain protein (18 kDa) that is expressed predominantly in steroid-synthesizing tissues. This protein has multiple functions including the regulation of steroidogenesis, in particular the production of neuroactive steroids such as allopregnanolone in the brain. Emapunil exerts anxiolytic effects not only in animal models, but also in human volunteers. As a ligand for TSPO, AC-5216 produces anxiolytic- and antidepressant-like effects in animal models. The antidepressant-like effects of AC-5216 on HFD-STZ rats, suggests that TSPO may represent a novel therapeutic target for depression in T2DM.


Kinase Assay: TSPO ligand XBD173 enhanced gamma-aminobutyric acid-mediated neurotransmission and counteracted induced panic attacks in rodents in the absence of sedation and tolerance development. XBD173 also exerted antipanic activity in humans and, in contrast to benzodiazepines, did not cause sedation or withdrawal symptoms


Cell Assay:

In VivoEAE was induced in 9–11-week-old mice by subcutaneous injection of an emulsion containing 150 μg proteolipid protein (PLP139–151) peptide (Eurogentec, Liège, Belgium) emulsified 1:1 in Complete Freund's Adjuvant (CFA) to each hind flank (100 μl by flank). The CFA is prepared from Incomplete Freund's Adjuvant (IFA) (Santa Cruz Biotechnology, INC, Heidelberg, Germany) with mycobacterium tuberculosis (Difco Laboratories, Franklin Lakes, NJ) at 5 mg/ml. Then, the mice received 200 ng pertussis toxin (Enzo lifes sciences, Lausen, Swiss) in 200 μl sterile phosphate-buffered saline (PBS) intraperitoneally (i.p.) on day 0 and day 2 post-immunization (D0 and D2). Control mice were immunized without PLP139–151 according to a similar schedule. Clinical evaluation of symptoms was performed daily according to the standard EAE grading scale. The standard grading scale ranges from 0 to 10; 0: No clinical signs; 1: Partially limp tail; 2: Paralyzed tail; 3: Hind limb paresis, uncoordinated movement; 4: One hind limb paralyzed; 5: Both hind limbs paralyzed; 6: Hind limbs paralyzed, weakness in forelimbs; 7: Hind limbs paralyzed, one forelimb paralyzed; 8: Hind limbs paralyzed, both forelimbs paralyzed; 9: Moribund; 10: Death. The first measurement of the disease was taken on the day of EAE-induction (D0), and all the subsequent measurements were recorded every 24 h until sacrifice, as well as measuring the weight of animals.


XBD173 was synthesized by our chemist partners (F. Hallé and F. Bihel) according to the experimental procedure reported by Zhang et al. The mice received i.p. injections (200 μl) of XBD173 at a dose of 10, 20 or 30 mg/kg (n = 26 for the groups 10 and 20 mg/kg, at the beginning of the experiments and n = 8 for the group 30 mg/kg), depending on the body weight, dissolved in hydroxypropyl cellulose (HPC) 0.3% (Alfa Aesar, Haverhill, Massachusetts, USA) and vehicle mice were injected with HPC 0.3% (n = 23, at the beginning of the experiments) according to a similar schedule. Mice were treated every two days from D4 until sacrifice.

Animal model EAE was induced in 9–11-week-old mice
Formulation & Dosage i.p. injections (200 μl) of XBD173 at a dose of 10, 20 or 30 mg/kg; dissolved in hydroxypropyl cellulose (HPC) 0.3%.
References Biochim Biophys Acta. 2017 Dec;1863(12):3016-3027.