MPO-IN-28
产品说明书
 |
同义名 : | - |
| CAS号 : | 37836-90-1 | |
| 货号 : | A1148094 | |
| 分子式 : | C11H13N5O | |
| 纯度 : | 98% | |
| 分子量 : | 231.25 | |
| MDL号 : | MFCD00475732 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The heme enzyme myeloperoxidase (MPO) participates in innate immune defense mechanism through formation of microbicidal reactive oxidants. MPO-IN-28 is a the first potent, selective and mechanism-based irreversible MPO inhibitor with IC50 value of 44nM. MPO-IN-28 achieved residual MPO activity without H2O2 by 84%, residual MPO activity with H2O2 by 4%, residual MPO activity with Cl−+ H2O2 by 5% at 5μM and inhibited LDL oxidation with IC50 value of 0.09μM. It dose-dependently inhibited MPO inside neutrophils with IC50 value of 93.1μM. MPO-IN-28 possesses the characteristic of blood−brain barrier permeability, human intestinal absorption and cell permeability. It inhibited in vitro growth of normal human dermal fibroblast with IC50 value 17μM[2]. | ||
| 作用机制 | MPO-IN-28 interacts with the active site of MPO and MPO uses hydrogen peroxide to oxidize MPO-IN-28 thereby irreversibly inactivating the enzyme.[2] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
4.32mL 0.86mL 0.43mL |
21.62mL 4.32mL 2.16mL |
43.24mL 8.65mL 4.32mL |
| 参考文献 |
|---|