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• 产品描述： Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM

• 靶点： IC50: 24 nM (glucocerebroside synthase);Transferase

• 体外研究：
  Eliglustat tartrate shows good potency with an IC50 of 24 nM and specificity against the target enzyme.Incubating K562 or B16/F10 cells for 72 h with increasing amounts of Genz-112638 (0.6-1000 nM) results in a dose-dependent reduction of cell surface levels of both GM1 and GM3. The mean IC50 value for inhibiting the cell surface presentation of GM1 in K562 cells was 24 nM (range 14-34 nM) and that for GM3 in B16/F10 cells was 29 nM (range 12-48 nM)

• 体内研究：
  Mice that received drug prior to significant accumulation of substrate (10 weeks of age) showed reduced levels of glucosylceramide and number of Gaucher cells in the spleen, lung and liver when compared to age-matched control animals

• 参考文献：
  1. McEachern KA, et al. A specific and potent inhibitor of glucosylceramide synthase for substrate inhibition therapy ofGaucher disease. Mol Genet Metab. 2007 Jul;91(3):259-68.

• 溶解性： soluble  in  DMSO

• 保存条件： -80℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.472 ml	12.36 ml	24.719 ml
  5 mM	0.494 ml	2.472 ml	4.944 ml
  10 mM	0.247 ml	1.236 ml	2.472 ml
  50 mM	0.049 ml	0.247 ml	0.494 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 *