VU0361737
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货号：A709934
同义名：
ML-128
VU 0361737 is a brain-penetrant and selective positive allosteric modulator of mGlu4 receptors with EC50 values of 240 nM.
VU0361737 化学结构
VU0361737 3D分子结构
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VU0361737 纯度/质量文件 产品仅供科研
货号：A709934
标准纯度：
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VU0361737 质控信息
VU0361737 生物活性
描述
VU0361737 is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 displays weak activity at mGlu5 and mGlu8 receptors and inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors. VU0361737 exhibits terminal elimination half-lives (rat 1.9 h) due to high plasma clearance (894 mL/min/kg) following Intraperitoneal injection ( rat 10 mg/kg)[3] [4]
VU0361737 参考文献
[1] Engers DW, Field JR, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-cetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011 Feb 24;54(4):1106-10.
[2] Engers DW, Niswender CM, et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4(mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
[3] Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8
[4] Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011 Feb 24;54(4):1106-10
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VU0361737 实验方案
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1mg
5mg
10mg
1 mM
5 mM
10 mM
3.81mL
0.76mL
0.38mL
19.03mL
3.81mL
1.90mL
38.07mL
7.61mL
3.81mL
VU0361737 技术信息
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