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VU0361737

VU0361737 (ML-128) 是一种高效选择性的，中枢神经系统渗透性的代谢型谷氨酸受体 4(mGluR4)正变构调节剂，对人类和大鼠 mGluR4作用的EC50值分别为 240 和 110 nM。它具有神经保护作用，有用于帕金森氏病的研究潜力。

CAS号

1161205-04-4

分子式

C13H11ClN2O2

主要靶点

GluR

仅限科研使用

Cat No : CM05102

Print datasheet

Synonyms

ML-128|VU 0361737

验证数据展示

  • CAS No.: 1161205-04-4

    VU0361737
    CAS#: 1161205-04-4

产品信息

VU 0361737 is a specific positive allosteric modulator (PAM) of mGlu4 receptor.The EC50 of VU 0361737 is 240 nM for the human receptors. The EC50 of VU 0361737 is110 nM for rat receptors.It exhibits weak activity at mGlu5 and mGlu8 receptors, and is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors, can penetrate into CNS.

CAS号 1161205-04-4
分子式 C13H11ClN2O2
主要靶点 GluR
主要通路 神经科学
分子量 262.69
纯度 99.09%， 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 ML-128|VU 0361737

靶点活性

mGluR4 (HμMan):240 nM(EC50)|mGluR4 (Rat ):110 nM(EC50)

体内活性

VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [1]

体外活性

VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [1]

溶解度

DMSO:26.3 mg/mL (100 mM)

参考文献

1.Engers DW, et al. J Med Chem, 2009, 52(14), 4115-4118.
2.Engers DW, et al. J Med Chem, 2011, 54(4), 1106-1110.

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