• 产品描述： A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases

• 靶点： IC50: 20 nM (E-selectin), 25 nM (ICAM-1);Integrin

• 体内研究：
  A-205804 (5 mg/kg; p.o.) shows a half-life of 1 hour for rat.A-205804 (10 mg/kg; p.o.; 3 times per week; for 2 weeks) attenuates the E-selectin expression on the endothelial vascular niche cells in mice. Animal Model: C57BL/6 mice Dosage: 10 mg/kg Administration: Oral administration, 3 times per week, for 2 weeks Result: Efficiently decreased the expression of E-selectin on the endothelial vascular niche cells Animal Model: Rat Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: t1/2 = 1 hour

• 参考文献：
  1. Stewart AO, et al. Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem. 2001 Mar 15;44(6):988-1002. 2. Morita K, et al. RUNX transcription factors potentially control E-selectin expression in the bone marrow vascular niche in mice. Blood Adv. 2018 Mar 13;2(5):509-515.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.329 ml	16.645 ml	33.289 ml
  5 mM	0.666 ml	3.329 ml	6.658 ml
  10 mM	0.333 ml	1.664 ml	3.329 ml
  50 mM	0.067 ml	0.333 ml	0.666 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 *