• 产品描述： CID-2858522 is an effective and specific antigen receptor-mediated NF-κB activation inhibitor (IC50: 70 nM).

• 靶点： NF-κB

• 体内研究：
  CID-2858522 exhibits nonlinear pharmacokinetics, showing higher serum levels at the 0.5 h measurement time for the 30 mg/kg dose compared to 50 mg/kg but displaying typical dose-dependent behavior when measured at t=3 h. The increasing accumulation seen at a dose of 50 mg/kg may be due to a depot effect created by CYP3A4 inhibition. The cohort exhibits clear signs of morbidity at t=3 h at the 50 mg/kg dose

• 细胞实验： Cell viability is estimated based on cellular ATP levels. HEK293 cells at a density of 10^5/mL are seeded at 90 μL per well in 96-well white plates and cultured overnight. Compounds (e.g., CID-2858522; 1 μM, 2 μM, 3 μM, and 4 μM) are added (5 μL in medium) to wells and cells are cultured for 16 h, Finally, 50 μL ATPlite solution is added to each well and luminescence activity is read using a luminometer

• 动物实验： Three male mice are subjected to CID-2858522 (single i.p doses at 10, 30, and 50 mg/kg). Blood is drawn at 0.5 and 3 h, and subsequent LC/MS analysis of pooled samples is performed to determine the overall blood levels of CID-2858522

• 参考文献：
  1. Peddibhotla S, et al. Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules. J Med Chem. 2010 Jun 24;53(12):4793-7. 2. Okolotowicz KJ, et al. Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activationpathway. Bioorg Med Chem. 2010 Mar 1;18(5):1918-24.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.148 ml	10.738 ml	21.476 ml
  5 mM	0.43 ml	2.148 ml	4.295 ml
  10 mM	0.215 ml	1.074 ml	2.148 ml
  50 mM	0.043 ml	0.215 ml	0.43 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 *