344458-19-1
344458-19-1 結構式
基本信息
PJ34(游離)
2-(二甲基氨基)-N-(6-氧代-5,6-二氫菲啶-2-基)乙酰胺
N-(6-氧代-5,6-二氫菲啶-2-基)-2-(N,N-二甲基氨基)乙酰胺
CS-856
PJ34(free base)
PJ34
PJ-34
PJ 34
2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide
N,N-Dimethyl-2-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide
N-(6-OXO-5,6-DIHYDRO-PHENANTHRIDIN-2-YL)-N,N-DIMETHYLACETAMIDE HCL
2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide
Acetamide, N-(5,6-dihydro-6-oxo-2-phenanthridinyl)-2-(dimethylamino)-
N-(6-Oxo-5,6-dihydrophenanthridin-2-yl)-2-(N,N-dimethylamino)acetamide
常見問題列表
|
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.