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• 产品描述： RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research

• 靶点： IC50: 4.0 nM (Btk) Kd: 0.31 nM (Btk);BTK

• 体外研究：
  RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM). In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486

• 体内研究：
  RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood

• 参考文献：
  1. Xu D, et al. RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. 2. Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104. 3. Mina-Osorio P, et al. Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase. Arthritis Rheum. 2013 Sep;65(9):2380-91.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.648 ml	8.241 ml	16.483 ml
  5 mM	0.33 ml	1.648 ml	3.297 ml
  10 mM	0.165 ml	0.824 ml	1.648 ml
  50 mM	0.033 ml	0.165 ml	0.33 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 *