PJ-34 HCl - CAS:344458-15-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	PJ-34 HCl 促销
英文名称:	PJ-34 HCl
别名:	2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide hydrochloride
CAS No:	344458-15-7	分子式:	C₁₇H₁₈ClN₃O₂	分子量:	331.80
CAS No:	344458-15-7
分子式:	C₁₇H₁₈ClN₃O₂
分子量:	331.80

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P10090 PJ-34 HCl ≥98%(HPLC) (psaitong)

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包装规格：

10mg 25mg 100mg in glass bottle

溶解性：

溶于水（22mg/mL）和DMSO

产品描述：

基本信息

产品编号：P10090
产品名称：PJ-34 HCl
CAS:	344458-15-7	储存条件	粉末	-20℃	四年

分子式：	C17H18ClN3O2		溶于液体	-80℃	两年
分子量	331.80			-20℃	一个月
化学名：	2-(Dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide hydrochloride
Solubility (25°C)	体外	DMSO	66mg/mL (198.91mM)
		Ethanol	66mg/mL (198.91mM)
		Water	Insoluble
	体内（现配现用）	30% PEG400+0.5% Tween80+5% propylene glycol	15 mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.0139mL	15.0693mL	30.1386mL
5mM	0.6028mL	3.0139mL	6.0277mL
10mM	0.3014mL	1.5069mL	3.0139mL
50mM	0.0603mL	0.3014mL	0.6028mL

生物活性

产品描述	一种有效的细胞渗透性PARP抑制剂，EC5050：20nM。
靶点/IC₅₀	PARP (Cell-free assay) 20nM(EC50)
体外研究	PJ34 inhibits the PARP enzyme activity with an IC50 of 110±1.9nM. 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.
体内研究	To compare the potency and efficacy with other PARP inhibitors, PJ34 is evaluated at the doses of 3.2 and 10mg/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 (25mg/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-1mRNA by 54%, compared to vehicle-treated ischemic mice

推荐实验方法(仅供参考)

激酶实验：

Kinase Assay

To assess the PARP-1 or PARP-2 inhibitory activity of FR247304, 3-AB, and PJ34, PARP activity is evaluated with minor modifications. PARP enzyme assay is carried out in a final volume of 100μL consisting of 50mM Tris-HCl (pH 8.0), 25mM MgCl2, 1 mM dithiothreitol, 10μg activated salmon sperm DNA, 0.1μCi of [adenylate-32P]NAD, 0.2 units of recombinant human PARP for PARP-1 assay or 0.1 units of recombinant mouse PARP-2 for PARP-2 assay, and various concentrations of FR261529 or 3-AB. The reaction mixture is incubated at room temperature (23°C) for 15 min, and the reaction is terminated by adding 200μL of ice-cold 20% trichloroacetic acid (TCA) and incubated at 4°C for 10 min. The precipitate is transferred onto GF/B filter and washed three times with 10% TCA solution and 70% ethanol. After the filter is dried, the radioactivity is determined by liquid scintillation counting.

细胞实验:

Cell Assay

PC12 cell cultured are grown in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 5% (v/v) horse serum, and a 1% (v/v) penicillin-streptomycin antibiotics mixture. Cells are grown in an atmosphere of 95% air and 5% CO2 at 37°C. For all experiment, cells are seeded at a density of 4×104 cells/well in 96-well culture plates and allowed to attach overnight. For assessment of cell viability, hydrogen peroxide-induced cytotoxicity is quantified by a standard measurement of LDH release with the use of the LDH assay kit. Briefly, 6 h after hydrogen peroxide exposure, 20μL of medium of each well is collected, and the solution prepared from LDH assay kit is added. After incubation at room temperature for 30 min, the reaction is stopped by addition of 1 N HCl, and absorbance is measured at 450nm using a microplate reader.

动物实验:

Animal Administration

Rats

For transient focal ischemia, 9- to 10-week-old male Wistar rats (weighing 274-380g) are used. FR247304, PJ34, or 3-AB, which is suspended with 0.5% methylcellulose, is administered at doses of 10 and 32mg/kg for FR247304, 3.2 and 10mg/kg for PJ34, or 32 and 100mg/kg for 3-AB intraperitonially twice at 10 min before MCA occlusion and 10 min before recirculation. The administration volume is adjusted to 2mL/kg.

Mice

Male Swiss albino mice (27-32 g) are used. The PARP inhibitor, PJ34 (1.25, 12.5 or 25mg/kg) is dissolved in isotonic saline (NaCl, 0.9%) and injected intraperitoneally, in a volume of 10mL/kg, 15min before ischemia and again 4h after the onset of ischemia. Control ischemic mice and sham animals are given vehicle (saline). Naive animals are also included in the studies.

保存条件：

-20℃

UN码：

HazardClass：

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