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AZD7325
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。
AZD7325图片
CAS NO:942437-37-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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 ofGABAAα2 and Aα3 receptor(Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes[1][4]. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro[2]. AZD7325 has the potential for the investigation of anxiety and dravet syndrome[3]. PAM: positive allosteric modulator.

IC50& Target[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)[4].
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[2].
AZD7325 (0-10 μM; 3 consecutive days; once daily) causes CYP1A2 and CYP3A4 protein expression in human hepatocytes from donor HH210[2].

RT-PCR[2]

Cell Line:Primary human hepatocytes from one female (HH210) and two male (HH215, HH216) donors
Concentration:0.01, 0.1, 1, 10 μM
Incubation Time:3 consecutive days
Result:Led to increase of CYP1A2 mRNA expression

Western Blot Analysis[2]

Cell Line:Primary human hepatocytes from donors
Concentration:0.01, 0.1, 1, 10 μM
Incubation Time:3 consecutive days
Result:Increased CYP1A2 and CYP3A4 protein level.
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℃ for 10 mg/kg, 43.3℃ for 17.8 mg/kg, and 43.4℃ for 31.6 mg/kg compares to 42.2℃ in vehicle group[3].

Animal Model:Male and female P18 - P20 F1.Scn1a+/-mice[3]
Dosage:10, 17.8 or 31.6 mg/kg
Administration:Oral administration; 30 minutes before the induction of hyperthermia
Result:Attenuated hyperthermia-induced seizures in F1.Scn1a+/-mice with no sedative effect.
Clinical Trial
分子量

354.38

性状

Solid

Formula

C19H19FN4O2

CAS 号

942437-37-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(705.46 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8218 mL14.1091 mL28.2183 mL
5 mM0.5644 mL2.8218 mL5.6437 mL
10 mM0.2822 mL1.4109 mL2.8218 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.87 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.87 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。