2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. AZD6538

AZD6538 是一种有效、选择性和脑渗透性的 mGluR5 负变构调节剂。AZD6538 抑制 DHPG (HY-12598A) 刺激的表达大鼠或人类 mGluR5 的 HEK 细胞内 Ca2+ 释放，对大鼠 mGluR5 和人类 mGluR5 的 IC50 值分别为 3.2 和 13.4 nM。AZD6538 可用于神经性疼痛的研究。

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AZD6538 Chemical Structure

AZD6538 Chemical Structure

CAS No. : 453566-30-8

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AZD6538 相关抗体

Top Publications Citing Use of Products

查看 mGluR 亚型特异性产品:

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain[1].

IC50 & Target

rat mGluR5

3.2 ± 0.1 nM (IC50)

human mGluR5

13.4 ± 1.3 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
13.4 nM
Compound: 3, AZD-6538
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]
HEK293 IC50
3.2 nM
Compound: 3, AZD-6538
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
51 nM
Compound: 3, AZD-6538
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]
体外研究
(In Vitro)

AZD6538 以浓度依赖性方式完全逆转了人类 mGluR5-GHEK 细胞中谷氨酸刺激的 (EC80, 80 μM) 磷脂酰肌醇水解，IC50 为 51 ± 3 nM[1]。

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

AZD6538 相关抗体:
分子量

291.24

Formula

C15H6FN5O
CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 4 mg/mL (13.73 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 3.4336 mL 17.1680 mL 34.3359 mL
5 mM 0.6867 mL 3.4336 mL 6.8672 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 (protect from light)。-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

AZD6538 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 (protect from light)。-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 3.4336 mL 17.1680 mL 34.3359 mL 85.8399 mL
5 mM 0.6867 mL 3.4336 mL 6.8672 mL 17.1680 mL
10 mM 0.3434 mL 1.7168 mL 3.4336 mL 8.5840 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:

AZD6538453566-30-8AZD 6538AZD-6538mGluRMetabotropic glutamate receptorsbrain penetrantneuropathic painphosphatidyl inositolInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-119282
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