| 中文名称 | PJ-34 |
| 英文名称 | PJ-34 |
| CAS号 | 344458-19-1 |
| 分子式 | C17H17N3O2 |
| 分子量 | 295.34 |
| EINECS号 | 604-604-1 |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 颜色 | 浅黄至卡其色 |
|
PARP 110 nM (IC 50 ) |
PARP-2 86 nM (IC 50 ) |
PARP-1 110 nM (IC 50 ) |
PJ34 inhibits the PARP enzyme activity with an IC 50 of 110±1.9 nM. To compare the neuroprotective properties of other PARP inhibitors in PC12 cells, PJ34 is evaluated using by LDH assay. PJ34 treatment also significantly and concentration dependently attenuates cell death at a concentration ranging from 10 -7 to 10 -5 M.
To compare the potency and efficacy with other PARP inhibitors, PJ34 is evaluated at the doses of 3.2 and 10 mg/kg, respectively. PJ34 at the dose of 3.2 mg/kg significantly reduces cortical damage by 33%; however, 10 mg/kg dosing shows reversed effect (17% reduction). PJ34 (25 mg/kg) reduces the levels of TNF-α mRNA in ischemic animals by 70% and these values in treated mice do not differ from that of sham or naive animals. Treatment of ischemic mice with PJ34 reduces the level of E-selectin mRNA by 81% and that of ICAM-1 mRNA by 54%, compared to vehicle-treated ischemic mice.