AZD7325
目录号: PL01865 纯度: ≥99%
CAS No. :942437-37-8
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中文名称
AZD7325
英文名称
AZD7325
英文别名
KNM216XOUH;4-amino-8-(2-fluoro-6-methoxyphenyl)-N-propylcinnoline-3-carboxamide;AZD7325;KYDURMHFWXCKMW-UHFFFAOYSA-N;GTPL7712;BCP29554;AZD 7325;BDBM50418481;AZD 7325; AZD7325;SB17497;DB13994;Q27074785;4-Amino-8-(2-fluoro-6-methoxy-phenyl)-N-propylcinnoline-3-carboxamide;4-amino-8-(2-fluoro-6-methoxy-phenyl)-N-propyl-cinnoline-3-carboxamide;4-Amino-8-(2-fluoro-6-methoxyphenyl)-N-propyl-3-cinnolinecarboxamide (ACI);AZD-7325
Cas No.
942437-37-8
分子式
C19H19FN4O2
分子量
354.38
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
AZD7325 是具有口服活性的 α2,3 receptor 的正向别构调节剂 (PAM),Ki 分别是 0.3 and 1.3 nM,但在 α1 和 α5 受体亚型上效果较差。AZD7325 是一种中等 CYP1A2 和强效 CYP3A4 诱导剂。AZD7325 具有用于焦虑和 dravet 综合征相关研究的潜力。
生物活性
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (K i =0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
性状
Solid
IC50 & Target[1][2]
CYP1A2 CYP3A4
体外研究(In Vitro)
AZD7325 is a high affinity and selective modulator of the GABAA receptor system, exhibits high binding affinity at GABAAα1, α2 and α3 (Ki=0.5, 0.3, and 1.3 nM, respectively), and low at GABAAα5 (Ki=230 nM).
AZD7325 (0-10 μM; 3 consecutive days; once daily) causes a maximal CYP1A2 mRNA expression of 3.2-fold, 2.1-fold, and 2.5-fold in human hepatocytes from donor HH210, HH215, and HH216, respectively.
AZD7325 (0-10 μM; 3 consecutive days; once daily) causes CYP1A2 and CYP3A4 protein expression in human hepatocytes from donor HH210.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
AZD7325 (oral administration; 10, 17.8 or 31.6 mg/kg; 30 minutes before the induction of hyperthermia) attenuates hyperthermia-induced seizures, shows median thresholds in the treatment groups of 42.8°C for 10 mg/kg, 43.3°C for 17.8 mg/kg, and 43.4°C for 31.6 mg/kg compares to 42.2°C in vehicle group.
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
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Chen X, et al. The central nervous system effects of the partial GABA-Aα2,3 -selective receptor modulator AZD7325 in comparison with lorazepam in healthy males.Br J Clin Pharmacol. 2014 Dec;78(6):1298-314.
[2]. Zhou D, et al. A clinical study to assess CYP1A2 and CYP3A4 induction by AZD7325, a selective GABA(A) receptor modulator - an in vitro and in vivo comparison.Br J Clin Pharmacol. 2012 Jul;74(1):98-108.
溶解度数据
In Vitro: DMSO : 100 mg/mL (282.18 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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