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

AZD 9272 是一种选择性、口服活性且可透过血脑屏障的 mGluR5 拮抗剂,对大鼠和人受体的IC50 分别为 2.6 nM 和 7.6 nM。AZD 9272 的选择性比其他 mGlu 受体高出 3900 倍以上。

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AZD 9272 Chemical Structure

AZD 9272 Chemical Structure

CAS No. : 327056-26-8

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Other Forms of AZD 9272:

  • 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 selective, orally active and brain penetrant mGluR5 antagonist with IC50s of 2.6 nM and 7.6 nM for rat and human receptors, respectively. AZD 9272 shows >3900-fold selectivity over other mGlu receptors[1]2].

IC50 & Target[2]

rat mGluR5

2.6 nM (IC50)

human mGluR5

7.6 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
2.6 nM
Compound: 2, AZD-9272
Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
[PMID: 23046966]
HEK293 IC50
26 nM
Compound: 2, AZD-9272
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challen
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challen
[PMID: 23046966]
HEK293 IC50
7.6 nM
Compound: 2, AZD-9272
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
[PMID: 23046966]
体外研究
(In Vitro)

AZD 9272 会导致人类和大鼠表达 mGluR5 的细胞系中,对 1.5 μM mGluR I 组选择性激动剂 DHPG 的细胞内 Ca2+ 反应强度呈浓度依赖性下降。最大抑制率为 100%。随着 AZD9272 浓度的增加,DHPG 的效力和最大反应降低。AZD9272 以浓度依赖性方式完全逆转人类 mGluR5-GHEK 细胞中谷氨酸刺激的(EC80,80 μM)磷脂酰肌醇水解,IC50 为 26 nM[2]

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

体内研究
(In Vivo)

AZD 9272 单次静脉注射 3 μmol/kg 后清除率较低,其从血浆中消除的终末半衰期为 2 至 6 小时。口服给药后的终末半衰期与静脉给药后的半衰期相似。AZD9272 的稳态分布容积处于中等水平[1]
2.84 mg/kg 的 AZD9272 在给药后 20 小时内可引起超过 80%、通常超过 99% 的中期有效剂量 (MTEP) 适当反应,给药后 24 小时下降至约 20%,t1/2 为 21.93 小时,并且对缓解率没有系统性影响。 AZD9272 首次引起 >90% MTEP 适当反应的时间点是给药后 30 分钟[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
细胞实验: 

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

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

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.

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产品名称:
AZD 9272
目录号:
HY-110254
需求量: