|N-(4-氯-3-甲氧基苯基)-2-吡啶甲酰胺|CsnPharm

CAS No.: 1161205-04-4

VU0361737 Catalog No. CSN15882

Synonyms: ML-128

VU 0361737 is a brain-penetrant and selective positive allosteric modulator of mGlu4 receptors with EC50 values of 240 nM.

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8068 mL
- 19.0338 mL
- 38.0677 mL
- 5 mM
- 0.7614 mL
- 3.8068 mL
- 7.6135 mL
- 10 mM
- 0.3807 mL
- 1.9034 mL
- 3.8068 mL

技术信息

CAS号

1161205-04-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H11ClN2O2

运输

蓝冰

分子量

262.69

别名

ML-128

溶解度

DMSO	53.0 mg/mL (201.8 mM)
Water	Insoluble
Ethanol	Insoluble

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