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344458-15-7

中文名稱 PJ34
英文名稱 PJ-34
CAS 344458-15-7
分子式 C17H17N3O2HCl
MOL 文件 344458-15-7.mol
更新日期 2024/12/17 19:34:11
344458-15-7 結(jié)構式 344458-15-7 結(jié)構式

基本信息

中文別名
PJ 34 鹽酸鹽
PARPL和PARP2抑制劑
N-(6-氧代-5,6-二氫菲啶-2-基)-2-(N,N-二甲基氨基)乙酰胺鹽酸鹽
英文別名
PI34
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%
所屬類別
生物化工:PARP 抑制劑

物理化學性質(zhì)

儲存條件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度H2O:可溶,22mg/mL
形態(tài)白色固體
顏色白色到黃色
敏感性Light Sensitive & Hygroscopic
穩(wěn)定性從購買之日起 2 年內(nèi)保持穩(wěn)定。 DMSO 或蒸餾水中的溶液可在 -20℃ 下儲存長達 3 個月。

安全數(shù)據(jù)

安全說明22-24/25
WGK Germany3
海關編碼29339900

圖譜信息

常見問題列表

生物活性
PJ34 hydrochloride 是 PARP1/2 的抑制劑,IC50 值分別為 110 nM 和 86 nM。
靶點

PARP

110 nM (IC 50 )

PARP-2

86 nM (IC 50 )

PARP-1

110 nM (IC 50 )

體外研究

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.

體內(nèi)研究

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.

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