2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. AZD 9272

AZD 9272 是一种脑渗透性 mGluR5 拮抗剂。

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AZD 9272 Chemical Structure

AZD 9272 Chemical Structure

CAS No. : 327056-26-8

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1 mg ￥1059
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AZD 9272 相关抗体

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD 9272 is a brain penetrant mGluR5 antagonist.

IC50 & Target[1]

mGluR5

 

体外研究
(In Vitro)

AZD 9272 causes a concentration dependent decrease in the magnitude of the intracellular Ca2+ response to 1.5 μM of the mGluR group I selective agonist DHPG in both the human and the rat mGluR5 expressing cell lines. The maximal inhibition is 100%. The mean IC50 (±SD) value at the human mGluR5 is 7.6±1.1 nM (n=13) for AZD9272. The mean IC50 value at the rat mGluR5 is 2.6±0.3 nM (n=3) for AZD9272. In contrast, 10 μM of AZD9272 does not diminish the response to 10 μM ATP in the background GHEK cells. Increasing concentrations of AZD9272 causes a decrease in the potency and the maximal response of DHPG. AZD9272 completely reverses the glutamate-stimulated (EC80, 80 μM) phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells in a concentration-dependent manner, with IC50 of 26±3 nM (n=21)[1].

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

AZD 9272 相关抗体:
体内研究
(In Vivo)

The clearance of AZD 9272 is low following a single intravenous dose at 3 μmol/kg and AZD 9272 is eliminated from plasma with terminal half-lives between 2 and 6 h. The terminal half-lives following oral dosing are similar to the half-lives following intravenous dosing. The volume of distribution at steady state is intermediate for AZD9272[1]. AZD9272 causes no cocaine-appropriate responding and causes a non-dose-dependent reduction in response rates at higher doses. AZD9272 at 2.84 mg/kg causes greater than 80% and typically more than 99% MTEP-appropriate responding up to 20 hours after dose, with a decline to approximately 20% at 24 hours after dose, yielding a t1/2 of 21.93 hours, and causes no systematic effects on response rates. The first time point at which AZD9272 causes >90% MTEP-appropriate responding is at 30 minutes after dose[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

284.22

Formula

C14H6F2N4O
CAS 号
性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 2 mg/mL (7.04 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5184 mL 17.5920 mL 35.1840 mL
5 mM 0.7037 mL 3.5184 mL 7.0368 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Kinase Assay
[1]

Saturable binding and competition binding studies utilize incubations of 1 hour at 22°C. For saturation studies, membranes from mGluR5-GHEK cells are incubated with increasing concentrations (0.1 to 30 nM) of [3H]AZD9272, in the presence or absence of 10 μM MPEP. In a variation of these studies, saturable [3H]AZD9272 binding is determined in the presence of low concentrations (10 and 20 nM) of MPEP. Consistency of the Bmax in the presence or absence of MPEP supports the interaction of these ligands with a unitary binding site[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

hmGluR5-GHEK cells are seeded onto 96 well plates at 50,000 cells/well in media containing 10 µCi/mL [3H]myo-inositol. Cells are incubated overnight (16 h), then washed three times and incubated for 1 hour at 37°C in HEPES buffered saline supplemented with 1 unit/mL glutamate pyruvate transaminase and 2 mM pyruvate. Cells are washed once in HEPES buffered saline and pre-incubated for 10 minutes in HEPES buffered saline containing 10 mM LiCl. Antagonist activity is determined by pre-incubating cells with AZD9272 for 10 minutes, then incubating for 30 minutes at 37°C in the presence of glutamate (EC80, 80 µM). AZD9272 is tested at 10 concentrations between 1 nM and 30 μM, in duplicate. The reaction is terminated by the addition of 0.1 mL perchloric acid (5%) on ice, with incubation at 4°C for at least 30 minutes[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Approximately 48 male Wistar rats weighing 240 to 250 g at the beginning of the experiments are housed in pairs, or group housed up to 8 rats per cage, in a colony room with water accessible at all times and lights on between 6:00 AM and 6:00 PM; by restricting access to food, animals are kept at approximately 80% of free feeding weight. All animals are divided into different groups and trained to discriminate cocaine (3.4 mg/kg i.p., 15 minutes), PCP (1.6 mg/kg i.p., 30 minutes), MTEP (2 mg/kg i.p., 30 minutes), or AZD9272 (1.6 mg/kg p.o., 60 minutes) from no drug[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

AZD 9272 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5184 mL 17.5920 mL 35.1840 mL 87.9600 mL
5 mM 0.7037 mL 3.5184 mL 7.0368 mL 17.5920 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD 9272327056-26-8AZD9272AZD-9272mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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产品名称：
AZD 9272
目录号：
HY-110254
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