同义名 :	ML-128
	CAS号 :	1161205-04-4
	货号 :	A709934
	分子式 :	C13H11ClN2O2
	纯度 :	99%+
	分子量 :	262.69
	MDL号 :	MFCD16618402
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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]. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research. VU0361737 (1-10 μM) partially attenuates the Staurosporine (HY-15141)- and Doxorubicin (HY-15142)-evoked cell death on human neuroblastoma SH-SY5Y cells[4].

实验方案
	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

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