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• 产品描述： Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.

• 靶点： JAK2:1 nM (IC50);Tyk2:1 nM (IC50);JAK3:5 nM (IC50);Murine JAK1:15 nM (IC50);CDK2:3.3 μM (IC50);cAMP-dependent kinase:7.1 μM (IC50);Csk:2.1 μM (IC50);Hck:7.7 μM (IC50);Fyn T:0.5 μM (IC50);p38:11 μM (IC50);MAPK:1.78 μM (IC50);Mek:0.16 μM (IC50);IκB Kinase 2:0.3 μM (IC50);KDR:1.4 μM (IC50);Flt-1:1.52 μM (IC50);Flt-4:0.69 μM (IC50);FGFR:1.48 μM (IC50);FGFR2:0.94 μM (IC50);Tek:24 μM (IC50);PDGFR:1.49 μM (IC50);PKC(α):1.2 μM (IC50);TyrosineKinases;JAK

• 体内研究：
  Pyridone 6 (P6) delays the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. P6-nano strongly ameliorates atopic dermatitis (AD) in NC/Nga mice, exerting an effect comparable to that of betamethasone ointment, a commonly used drug, which also tested as a positive control. In contrast, empty polylactic acid with glycolic acid (PLGA) nanoparticles (C-nano) seemed to have no effect[

• 参考文献：
  1. Thompson JE, et al. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23. 2. Nakagawa R, et al. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17. J Immunol. 2011 Nov 1;187(9):4611-20.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.233 ml	16.163 ml	32.327 ml
  5 mM	0.647 ml	3.233 ml	6.465 ml
  10 mM	0.323 ml	1.616 ml	3.233 ml
  50 mM	0.065 ml	0.323 ml	0.647 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 *