Emapunil

目录号: PL11760 纯度: ≥99%
Emapunil (AC-5216) 是口服有效的、选择性的 TSPO (一种线粒体苯二氮受体) 的配体,在多种动物模型中表现出抗焦虑和抗抑郁活性。
CAS No. :226954-04-7
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中文名称
Emapunil
中文别名
依马普尼
英文名称
Emapunil
英文别名
9H-Purine-9-acetamide,N-ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-;AC 5216;AC-5216;Emapunil;N-BENZYL-N-ETHYL-2-(7-METHYL-8-OXO-2-PHENYL-7H-PURIN-9(8H)-YL)ETHANAMIDE;N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenylpurin-9-yl)acetamide;AC1O5FL9;CHEBI:597751;CHEMBL513922;CTK4E9959;SureCN4757030;UNII-OG837L732J;XBD-173;N-Ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-9H-purine-9-acetamide;NVP-XBD173;9H-Purine-9-acetamide, N-ethyl-7,8-dihydro-7-methyl-8-oxo-2-phenyl-N-(phenylmethyl)-;émapunil;emapunilo;emapunilum;N-Benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamid;N-Benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide;N-Benzyl-N-éthyl-2-(7-méthyl-8-oxo-2-phényl-7,8-dihydro-9H-purin-9-yl)acétamide;XBD173;ac5216;AC-5216;XBD-173;emapunil(ac-5216);N-(benzyl)-N-ethyl-2-(8-keto-7-methyl-2-phenyl-purin-9-yl)acetamide;n-benzyl-n-ethyl-2-(7-methyl-8-oxo-2-phenyl-7h-purin-9(8h)-yl)acetamide;N-ethyl-2-(7-methyl-8-oxo-2-phenyl-9-purinyl)-N-(phenylmethyl)acetamide;N-ethyl-2-(7-methyl-8-oxo-2-phenylpurin-9-yl)-N-(phenylmethyl)acetamide;N-ethyl-2-(7-methyl-8-oxo-2-phenyl-purin-9-yl)-N-(phenylmethyl)acetamide;N-ethyl-2-(7-methyl-8-oxo-2-phenyl-purin-9-yl)-N-(phenylmethyl)ethanamide;SX-5216;UO7100000;XBD173 |
Cas No.
226954-04-7
分子式
C23H23N5O2
分子量
401.46
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述

Emapunil (AC-5216) 是口服有效的、选择性的 TSPO (一种线粒体苯二氮受体) 的配体,在多种动物模型中表现出抗焦虑和抗抑郁活性。

产品详情
Emapunil (AC-5216) 是口服有效的、选择性的 TSPO (一种线粒体苯二氮受体) 的配体,在多种动物模型中表现出抗焦虑和抗抑郁活性。
生物活性
Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models.
性状
Solid
体内研究(In Vivo)
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.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Atsuko Kita, et al. Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand. Br J Pharmacol. 2004 Aug;142(7):1059-72.
[2]. Marcus Karlstetter, et al. Translocator protein (18 kDa) (TSPO) is expressed in reactive retinal microglia and modulates microglial inflammation and phagocytosis. J Neuroinflammation. 2014 Jan 8;11:3.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (83.02 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Atsuko Kita, et al. Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand. Br J Pharmacol. 2004 Aug;142(7):1059-72.
[2]. Marcus Karlstetter, et al. Translocator protein (18 kDa) (TSPO) is expressed in reactive retinal microglia and modulates microglial inflammation and phagocytosis. J Neuroinflammation. 2014 Jan 8;11:3.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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