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• 产品描述： ML355是有效的选择性h12-LOX抑制剂，IC50为290 nM

• 靶点： 12-LOX;Lipoxygenase

• 体外研究：
  ML355 displays nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases

• 体内研究：
  In vivo PK studies where ML355 is administered as a solution via IV (3mpk) and PO (30mpk) demonstrated that ML355 is orally bioavailable (%F = 20) with good half-life (T1/2 = 2.9 hours). At 30 mpk dosing, ML355 achieves a Cmax of over 135 times the in vitro IC50 and remains over IC50 value for over 12 hours. The compound has low clearance (3.4 mL/min/kg) and good overall exposure (AUCinf) of 38 µM. Although, the volume of distribution (VD) observed is low (0.55 L/kg), the rest of the PK profiling results suggest a reasonable distribution between tissue and blood

• 细胞实验： Cell lines: U87 cells Concentrations: 10 µM Incubation Time: 24 h Method: Cells were treated with indicated concentration of drug for 24 h.

• 动物实验： Animal Models: C57BL/6 mice Dosages: 15 or 30 mg/kg Administration: p.o.

• 参考文献：
  1. Luci D, et al. Discovery of ML355, a Potent and Selective Inhibitor of Human 12-Lipoxygenase. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2013 Apr 12 [updated 2014 Sep 18]. 2. Yang X, et al. miR-18a promotes glioblastoma development by down-regulating ALOXE3-mediated ferroptotic and anti-migration activities. Oncogenesis. 2021 Feb 12;10(2):15. 3. Adili R, et al. First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis. Arterioscler Thromb Vasc Biol. 2017 Oct;37(10):1828-1839.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.265 ml	11.324 ml	22.649 ml
  5 mM	0.453 ml	2.265 ml	4.53 ml
  10 mM	0.226 ml	1.132 ml	2.265 ml
  50 mM	0.045 ml	0.226 ml	0.453 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 *