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AZD-8529 mesylate

AZD-8529 mesylate 是高度选择性的可口服mGluR2正向调节剂，EC50值为 285 nM。它在 20-25 M 时，对 mGluR1、3、4、5、6、7 和 8 亚型没有显示正变构调节剂反应。

CAS号

1314217-69-0

分子式

C25H28F3N5O6S

主要靶点

GluR

仅限科研使用

Cat No : CM05084

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Synonyms

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  • CAS No.: 1314217-69-0

    AZD-8529 mesylate
    CAS#: 1314217-69-0

产品信息

AZD-8529 mesylate is a highly selective, and orally bioavailable positive allosteric modulator of mGluR2 (EC50: 285 nM). It shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

CAS号 1314217-69-0
分子式 C25H28F3N5O6S
主要靶点 GluR
主要通路 神经科学
分子量 583.58
纯度 99.50%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

mGluR2:（EC50）285 nM

体内活性

AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats. AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys.

体外活性

AZD-8529 potentiates the effects of glutamate at mGluR2 (EC50: 195 nM). It does not elicit antagonist responses on mGluRs at 25 μM.

溶解度

DMSO:41.67 mg/mL (71.40 mM),Sonification is recommended.

参考文献

1.Justinova Z, et al. The Novel Metabotropic Glutamate Receptor 2 Positive Allosteric Modulator, AZD8529, Decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. Biol Psychiatry. 2015 Oct 1;78(7):452-62.

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