|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|CsnPharm

CAS No.: 344458-15-7

PJ34 HCl/PJ34 盐酸 Catalog No. CSN13594

Synonyms: PJ-34 (hydrochloride);PJ-34;PJ-34 HCl

PJ34 HCl is a potent specific inhibitor of PARP-l/2 with IC50 of 110 nM and 86 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PARP1

EC50:20nM PARP2

EC50:20nM
描述PJ34 is a specific inhibitor of poly (ADP-ribose) polymerase 1, and is involved in immune regulation, may be effective in preventing acute cardiac rejection. Compared with the control group, In vitro, PJ34 (20 mg/kg/day) treatment reduced the proportion of CD4+ IFN-γ+ and CD4+ IL-17A+ cells and increased the percent of CD4+ IL-4+ and CD4+ Foxp3+ cells in the spleens. In vitro, PJ34 treatment significantly inhibited the mRNA levels of IFN-γ and IL-17A and promoted the mRNA levels of TGF-β and FOXP-3 in activated CD4+ T cells^[3]. In vivo, PJ34 (20 mg/kg/day) prevented HFD-induced atherosclerosis in the rabbits^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
Escherichia coli BL21 Star (DE3) cells	-	Function assay	-	Inhibition of 6xhis-tagged ARTD5 (unknown origin) expressed in Escherichia coli BL21 Star (DE3) cells, IC50=0.57 μM	24900770
Escherichia coli Rosetta2 (DE3) cells	-	Function assay	-	Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50=0.21878 μM	24900770
HeLa cells	-	Function assay	-	Inhibition of PARP1 in human HeLa cells by fluid scintillation counting using [adenylated-32P]NAD as substrate, IC50=0.02 μM	18713665

更多
动物研究
剂量
Rat: 10 mg/kg^[3] (i.v.); 30 mg/kg^[4] (p.o.) Mice: 1.5 mg/kg - 25 mg/kg^[5] (i.p.)

给药途径
i.v., p.o., i.p.
参考文献

动物研究
剂量	Rat: 10 mg/kg^[3] (i.v.); 30 mg/kg^[4] (p.o.) Mice: 1.5 mg/kg - 25 mg/kg^[5] (i.p.)
给药途径	i.v., p.o., i.p.

[1] Scott GS, Kean RB, et al. The therapeutic effects of PJ34 [N-(6-oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide.HCl] , a selective inhibitor of poly(ADP-ribose) polymerase, in experimental allergic encephalomyelitis are associated with immunomodulation. J Pharmacol Exp Ther. 2004 Sep;310(3):1053-61.
[2] Scott GS, et al. J Pharmacol Exp Ther, 2004, 310(3), 1053-1061.
[3] Chen X, Huang Y, Wang D, Dong N, Du X. PJ34, a PARP1 inhibitor, attenuates acute allograft rejection after murine heart transplantation via regulating the CD4+ T lymphocyte response. Transpl Int. 2021;34(3):561-571.
[4] Zha S, Wang F, Li Z, Ma Z, Yang L, Liu F. PJ34, a PARP1 inhibitor, promotes endothelial repair in a rabbit model of high fat diet-induced atherosclerosis. Cell Cycle. 2019;18(17):2099-2109.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0139 mL
- 15.0695 mL
- 30.1389 mL
- 5 mM
- 0.6028 mL
- 3.0139 mL
- 6.0278 mL
- 10 mM
- 0.3014 mL
- 1.5069 mL
- 3.0139 mL

技术信息

CAS号

344458-15-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H18ClN3O2

运输

蓝冰

分子量

331.80

别名

PJ-34 (hydrochloride);PJ-34;PJ-34 HCl

溶解度

DMSO	66.0 mg/mL (198.9 mM)
Water	65.0 mg/mL (195.9 mM)
Ethanol	Insoluble

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

15 mg/mL

suspension

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靶点	Description	IC50
PARP1		EC50:20nM
PARP2		EC50:20nM

PJ34 HCl/PJ34 盐酸 Catalog No. CSN13594

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