• 产品描述： ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 is potential for the treatment of epilepsy

• 靶点： EC50: 0.16 μM (GIRK1/2), 18 μM (GIRK1/4);PotassiumChannel

• 体外研究：
  ML 297 is completely inactive for GIRK2/3. ML297 shows concentration-dependent efficacy in expressing GIRK1/2 cells and with an EC50 of 162 nM. ML297 shows a complete inability to modulate the activity of HEK-293 cells expressing GIRK2 alone and GIRKGIRK2/3

• 体内研究：
  ML297 (60 mg/kg; i.p.) shows a highly significant ability to both prevent convulsions and prevent fatality of the PTZ treatment. Animal Model: 8-10 months old C57/BL6 male mice (approximately 30 g) Dosage: 60 mg/kg Administration: Intraperitoneal injection Result: Most of the animals neither convulsions nor death.

• 参考文献：
  1. Wen W, et al. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4562-6. 2. Kaufmann K, et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.046 ml	15.229 ml	30.458 ml
  5 mM	0.609 ml	3.046 ml	6.092 ml
  10 mM	0.305 ml	1.523 ml	3.046 ml
  50 mM	0.061 ml	0.305 ml	0.609 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *