| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京