AZD-8529
目录号: PL07154 纯度: ≥98%
CAS No. :1092453-15-0
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中文名称
AZD-8529
英文名称
AZD-8529
英文别名
AZD8529;6H81G454I7;7-methyl-5-[3-(piperazin-1-ylmethyl)-1,2,4-oxadiazol-5-yl]-2-[[4-(trifluoromethoxy)phenyl]methyl]-3H-isoindol-1-one;7-Methyl-5-(3-piperazin-1-ylmethyl-(1,2,4)oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one;7-methyl-5-(3-piperazin-1-ylmethyl-[1,2,4]oxadiazol-5-yl)-2-(4-trifluoromethoxybenzyl)-2,3-dihydroisoindol-1-one;GTPL7678;AZD 8529;BDBM501946;AZD-8529
Cas No.
1092453-15-0
分子式
C24H24F3N5O3
分子量
487.47
包装储存
Pure form -20°C 3 years;4°C 2 years
产品详情
AZD-8529 是一种有效的,高度选择性的,可口服的 mGluR2 正向调节剂,EC50 值为 285 nM;在 20-25 M 的浓度范围内,对 mGluR1,3,4,5,6,7 和 8 没有正向调节作用。
生物活性
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC 50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
性状
Oil
IC50 & Target[1][2]
mGluR2 285 nM (EC50)
体外研究(In Vitro)
AZD-8529 potentiates the effects of glutamate at mGluR2 with an EC50 of 195 nM.
AZD-8529 does not elicit antagonist responses on mGluRs at 25 μM.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys.
AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Justinova Z, et al. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (128.21 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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