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• 产品描述： Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.

• 靶点： EC50: 100 nM (TLR8)

• 体外研究： Among the TLRs tested (TLR2, 3, 4, 5, 7, 8, and 9), Motolimod (VTX-2337) selectively activates TLR8. Motolimod stimulates the production of both TNFα (EC50=140±30 nM based on 10 donors) and IL-12 (EC50=120±30 nM based on 10 donors) in PBMCs. The EC50 value for MIP-1β induction is 60 nM for Motolimod

• 体内研究： Monkeys receive a subcutaneous injection of Motolimod (1 or 10 mg/kg), and plasma is collected predose, 6, 12, 24, and 96 h post-injection. For the 10 mg/kg dose, mean plasma levels of IL-1β increase from baseline levels of 0.5 pg/mL, up to 9.12±2.7 ng/mL (p<0.05, t-test) at 6 h post-administration of Motolimod (10 mg/kg). Circulating levels of IL-18 also increase from a baseline of ~ 1 pg/mL to 68.7±4.4 pg/mL (p<0.05, t-test) at 6 h in response to the Motolimod (VTX-2337) treatment (10 mg/kg). Levels of IL-6 are monitored, as this mediator is induced in response to TLR8 activation, but the release is independent of NLRP3 inflammasome activation. In addition, plasma levels of IFNγ are assessed as a measure of NK cell activation in response to Motolimod treatment

• 参考文献：
  1. Lu H, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. 2. Dietsch GN, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.181 ml	10.903 ml	21.806 ml
  5 mM	0.436 ml	2.181 ml	4.361 ml
  10 mM	0.218 ml	1.09 ml	2.181 ml
  50 mM	0.044 ml	0.218 ml	0.436 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 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *