AZD7325|cas:942437-37-8|西域试剂

AZD7325,99.27%

产品编号：Bellancom-111052| CAS NO：942437-37-8| 分子式：C₁₉H₁₉FN₄O₂| 分子量：354.38

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-111052	￥1000.00	杭州北京（现货）
Bellancom-111052	￥1600.00	杭州北京（现货）
Bellancom-111052	￥4500.00	杭州北京（现货）
Bellancom-111052	￥6500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

AZD7325

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)，K_i 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^[4]. 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.

体外研究

AZD7325 is a high affinity and selective modulator of the GABAA receptor system, exhibits high binding affinity at GABAAα1, α2 and α3 (K_i=0.5, 0.3, and 1.3 nM, respectively), and low at GABAAα5 (K_i=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.
AZD7325 (0-10 µM; 3 consecutive days; once daily) causes CYP1A2 and CYP3A4 protein expression in human hepatocytes from donor HH210.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

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

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°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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female P18 - P20 F1.Scn1a^+/- mice
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female P18 - P20 F1.Scn1a^+/- mice
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female P18 - P20 F1.Scn1a^+/- mice
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (282.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8218 mL	14.1091 mL	28.2183 mL
5 mM	0.5644 mL	2.8218 mL	5.6437 mL
10 mM	0.2822 mL	1.4109 mL	2.8218 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。