| 產(chǎn)品描述： | VU0361737 (ML-128) 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 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research |
| 靶點(diǎn)： |
Human mGlu4:240 nM (EC50);Rat mGlu4:110 nM (EC50);GluR |
| 體內(nèi)研究： |
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) |
| 參考文獻(xiàn)： |
1. Engers DW, 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. 2. Engers DW, et al. 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 Ch 3. Jantas D, et al. Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation. Neurochem Int. 2015 Sep;88:124 |
| 溶解性： |
DMSO : 100 mg/mL (380.68 mM; Need ultrasonic) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.807 ml |
19.034 ml |
38.068 ml |
| 5 mM |
0.761 ml |
3.807 ml |
7.614 ml |
| 10 mM |
0.381 ml |
1.903 ml |
3.807 ml |
| 50 mM |
0.076 ml |
0.381 ml |
0.761 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。 |
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