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• 产品描述： VX-765 is an orally active IL-converting enzyme/caspase-1 inhibitor.

• 靶点： Caspase

• 体内研究：
  VRT-043198会抑制IL-1β从外周血单个核细胞和全血中的释放,IC50分别为0.67 μM和1.9 μM。VX-765是一种口服可吸收的VRT-043198前药,显示出对ICE /半胱天冬酶-1和半胱天冬酶-4的有效抑制作用,Ki分别为0.8 nM和<0.6 nM

• 细胞实验： VX-765 is solubilized in DMSO and stored, and then diluted with RPMI 1640 complete medium (DMSO 0.2%) before use[1]. A total of 2×105 cells/well (100 μL cell suspension) is distributed in triplicate in flat-bottom 96-well plates. Either 50 μL of VX-765 (40 μM in RPMI 1640 complete medium containing 0.2% DMSO) or vehicle control is added to appropriate wells. Following a 30-min incubation at 37°C, 50 μL of LPS diluted in RPMI 1640 complete medium is added at final concentrations varying from 0.001 to 10 ng/mL. Cells are returned to a 37°C incubator. At 4 h after LPS addition, 75 μL of supernatant is removed from wells, cleared by centrifugation for 5 min at 1500 rpm, and stored at 4°C until assayed. Cells are returned to a 37°C incubator until 24 h after LPS addition, at which time 100 μL of supernatant is removed, cleared by centrifugation, and stored at 4°C. Supernatants are tested using ELISA kits for IL-1β, IL-6, IL-18, and IL-1α

• 参考文献：
  1.Ravizza T, et al. Neurobiol Dis. 2008, 31(3), 327-333. 2.Maroso M, et al. Neurotherapeutics. 2011, 8(2), 304-315. 3.Wannamaker W, et al. J Pharmacol Exp Ther. 2007, 321(2), 509-516. 4.Akin D, et al. Neurobiol Dis. 2011, 44(3), 259-269. 5.Teng J F, Mei Q B, Zhou X G, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer[J]. MLA . Cancers. 2020, 12(1): 194.

• 溶解性： Ethanol:93  mg/mL  (182.7  mM)    DMSO:93  mg/mL  (182.7  mM)

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.965 ml	9.823 ml	19.646 ml
  5 mM	0.393 ml	1.965 ml	3.929 ml
  10 mM	0.196 ml	0.982 ml	1.965 ml
  50 mM	0.039 ml	0.196 ml	0.393 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 *