| 产品描述： | MPO-IN-28 is a novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM. |
| 靶点： |
Glutathione Peroxidase;GlutathionePeroxidase |
| 体外研究： |
5 μM of MPO-IN-28 was added to MPO in the presence of 30 μM of guaiacol. In the absence of H2O2, there was no inhibition of MPO, clearly underlining that MPO-IN-28 is an irreversible mechanism-based inhibitor. MPO-IN-28 inhibits the growth of normal human dermal fibroblast (NHDF) at a concentration (IC50) of 17 μM, which is about 400 times higher than the concentration of the MPO inhibitory effect (0.044 μM). |
| 细胞实验： |
To evaluate whether selected compounds exhibited toxicity at the cellular level at concentrations ranging from 0.005 to 50 μM, the colorimetric assay MTT was performed58 in normal human dermal fibroblasts (NHDF). Briefly, cell line was cultured in cell culture flasks, grown, and maintained at 37 °C, 95% humidity, 5% CO2 in fibroblast medium FBM supplemented with 2% fetal bovine serum, 0.1% insulin, rhFGF-B, and gentamicin and amphotericin. NHDF cells were chemically detached with trypsin and seeded in 96-well plates and left to attach for 24 h. Prior to treatment, compounds were dissolved in DMSO at a concentration of 10 mM, and cells were treated with the different concentrations of the compounds diluted in culture medium (5 nM to 50 μM) or left untreated for 72 h. The amount of viable cells was determined through the MTT mitochondrial reduction into formazan by living cells according to previously described.58 The optical density (OD) was measured in a Biorad 680RX plate reader at 570 nm (reference 630 nm), |
| 参考文献： |
1. Soubhye J, et al. Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. J Med Chem. 2017 Aug 10;60(15):6563-6586. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
4.324 ml |
21.621 ml |
43.243 ml |
| 5 mM |
0.865 ml |
4.324 ml |
8.649 ml |
| 10 mM |
0.432 ml |
2.162 ml |
4.324 ml |
| 50 mM |
0.086 ml |
0.432 ml |
0.865 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