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• 产品描述： BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease

• 靶点： IC50: 96 nM (mouse 11β-HSD1) IC50: 3341 nM (human 11β-HSD1);Dehydrogenase

• 体外研究：
  BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 µM) reduces MCP-1 expression in fully differentiation adipocytes. BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium in J774.1 macrophages by Elisa. RT-PCR Cell Line: Differentiation adipocytes Concentration: 100 μM Incubation Time: 24 hours Result: Down-regulated MCP-1 mRNA level.

• 体内研究：
  BVT-2733 (oral administration; 100 mg/kg; twice daily; 2 weeks) attenuates the arthritis severity and anti-CII level and decreases the levels of serum TNF-α, IL-1β, IL-6 and IL-17 in CIA mice. BVT 2733 (oral administration; 100 mg/kg; dosed (09.00 and 17.00 h); last 4 weeks) exhibits decreased body weight and enhanced glucose tolerance and insulin sensitivity when it compares to control mice. It also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo. Animal Model: Collagen-induced arthritis (CIA) mice Dosage: 100 mg/kg Administration: Oral administration; twice daily; 2 weeks Result: Reduced synovial inflammation and joint destruction. Animal Model: C57BL/6J mice Dosage: 100 mg/kg Administration: Oral administration; dosed (09.00 and 17.00 h); last 4 weeks Result: Improved metabolic homeostasis and suppressed the inflammation of adipose tissue in diet-induced obese mice.

• 参考文献：
  1. 11β-hydroxydehydrogenase 1 (11β-HSD1) Inhibitor in Development 2. Zhang L, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94. 3. Wang L, et al. BVT.2733, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, attenuates obesity and inflammation in diet-induced obese mice. PLoS One. 2012;7(7):e40056.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.331 ml	11.656 ml	23.312 ml
  5 mM	0.466 ml	2.331 ml	4.662 ml
  10 mM	0.233 ml	1.166 ml	2.331 ml
  50 mM	0.047 ml	0.233 ml	0.466 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 *