S80132
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- 公司名稱(chēng) 上海源葉生物科技有限公司
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- 更新時(shí)間 2025/5/16 7:52:56
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- 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)
- 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
- 溶解度： 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
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