344458-15-7
344458-15-7 结构式
基本信息
PARPL和PARP2抑制剂
N-(6-氧代-5,6-二氢菲啶-2-基)-2-(N,N-二甲基氨基)乙酰胺盐酸盐
CS-723
PJ34 HC
PJ34(HCL)
PJ 34
PJ-34
PJ34 hydrochL
PJ-34 USP/EP/BP
PJ 34 Hydrochloride
PARP Inhibitor VIII, PJ34
PJ34 hydrochloride, >=98%
物理化学性质
常见问题列表
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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.