• 产品描述： YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity

• 靶点： NLRP3:0.30 μM (IC50);IL-1β;ILReceptor; NOD-likeReceptor(NLR); NOD; Interleukin

• 体外研究：
  YQ128 (0.3-100 µM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59 µM. YQ128 (20 µM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells. Cell Viability Assay Cell Line: Mouse peritoneal macrophages Concentration: 0.3, 1.0, 3.0, 10, 30, 100 µM Incubation Time: 30 mins Result: Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC50 of 1.59 µM.

• 体内研究：
  YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration. YQ128 (oral; 20 mg/kg) shows delayed gastrointestinal absorption with a tmax and cmax of 12 h and 73 ng/mL, respectively. Oral bioavailability (Foral) is estimated as 10%. YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vdss) of 8.5 L/kg and rapid total clearance (CLtot) of 41 mL/min/kg. YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice. Animal Model: Sprague-Dawley rats (200-250 g) Dosage: 20 mg/kg (Pharmacokinetic Analysis) Administration: Iv Result: Had an intermediate terminal plasma half-life (t1/2) of 6.6 hours after iv administration.

• 参考文献：
  1. Jiang Y, et al. Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. J Med Chem. 2019 Oct 31.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.834 ml	9.172 ml	18.345 ml
  5 mM	0.367 ml	1.834 ml	3.669 ml
  10 mM	0.183 ml	0.917 ml	1.834 ml
  50 mM	0.037 ml	0.183 ml	0.367 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 *