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PJ34 Sale

(Synonyms: PJ-34;PJ 34) 目录号 : GC10995

An inhibitor of poly (ADP-ribose) polymerases

PJ34 Chemical Structure

Cas No.:344458-19-1

规格 价格 库存 购买数量
5mg
¥357.00
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10mg
¥462.00
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50mg
¥1,250.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Mouse endothelial cells and human umbilical vein endothelial cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.1 ~ 3 μM

Applications

In mouse endothelial cells, PJ34 significantly inhibited high glucose-induced PARP activation at the doses of 0.5 and 3 μM, as well as the development of endothelial dysfunction at the dose of 3 μM. Meanwhile, PARP inhibition caused by PJ34 (3 μM) did not alter the degree of NF-κB activation. In human umbilical vein endothelial cells, PJ34 at 1 μM exhibited marked inhibitory effect on high glucose-induced PARP activation.

Animal experiment [2]:

Animal models

MBP-immunized PLSJL mice

Dosage form

10 mg/kg; p.o.; b.i.d.

Applications

In MBP-immunized PLSJL mice, PJ34 inhibited the development of clinical signs of experimental allergic encephalomyelitis (EAE). PJ34 also suppressed the onset of EAE by reducing CNS inflammation and maintaining neurovascular integrity. In addition, PJ34 down-regulated the expression levels of TNF-α and ICAM-1 in the spinal cord tissues.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Garcia Soriano F, Virág L, Jagtap P, Szabó E, Mabley JG, Liaudet L, Marton A, Hoyt DG, Murthy KG, Salzman AL, Southan GJ, Szabó C. Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation. Nat Med. 2001 Jan;7(1):108-13.

[2]. Scott GS, Kean RB, Mikheeva T, Fabis MJ, Mabley JG, Szabó C, Hooper DC. 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.

产品描述

IC50 Value: 20 nM(EC50)[1] PJ34 (hydrochloride) is a novel potent specific inhibitor of PARP-l. PJ34 has been reported to enhance chemotherapeutic effects in certain types of tumors. in vitro: PJ34 inhibited peroxynitrite-induced cell necrosis with EC50 of 20 nM. PJ34 provides cardioprotection by decreasing myocardial infarct size and enhancing postischemic regional and global functional recovery [1]. Treatment with PJ34 increased NIS promoter activity without affecting PARP-1 binding to the promoter sequence, in addition to an increase of histone modification activation marks (H3K9K14ac, H3K4me3) [2]. in vivo: In a model of systemic endotoxemia, PJ34 pretreatment significantly reduced plasma levels of TNF-alpha, IL-1beta and nitrite/nitrate (breakdown products of nitric oxide) production. PJ34 treatment (oral gavage) induced a significant suppression of the inflammatory response in dextran sulfate colitis, multiple low dose streptozotocin diabetes [3]. The PJ34 showed significant reduction on infarct size (37.5%+/-4.5% and 50.5%+/-4.8% of the area at risk) for PJ34 and control pigs groups, respectively, (p < 0.05) [4]. Clinical trial: N/A

Chemical Properties

Cas No. 344458-19-1 SDF
别名 PJ-34;PJ 34
化学名 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide
Canonical SMILES CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32
分子式 C17H17N3O2 分子量 295.34
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.3859 mL 16.9296 mL 33.8593 mL
5 mM 0.6772 mL 3.3859 mL 6.7719 mL
10 mM 0.3386 mL 1.693 mL 3.3859 mL
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