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生物活性
PJ34 is a novel and potent inhibitor of poly(ADP-ribose) polymerase (PARP), an enzyme involved in DNA repair and cell proliferation, that dose-dependently inhibits purified PARP enzyme in a cell-free assay with half maximal effective concentration EC50 value of 20 nM. Unlike other PARP inhibitors (such as 3-AB), PJ34 does not possess any antioxidant properties but exhibits 10,000 times greater PARP inhibition than 3-AB (EC50 = 200 μM). PJ34 has been found to have neuro-protective effects and enhance the chemotherapeutic effects in several tumor types. Study results have shown that PJ34 inhibits peroxynitrite-induced cell necrosis with EC50 value of 20 nM and dose-dependently suppresses the growth of HepG2 cells.
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体外研究
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体内研究
30% PEG400+0.5% Tween80+5% Propylene glycol
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激酶实验
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细胞实验
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动物实验
10 mg/kg b.wt.每天两次 口服
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Garcia Soriano F, et al. Nat Med, 2001, 7(1), 108-113.
[2] Int. J. Mol. Med. 7, 255. Garcia-Soriano, F.G., et al. 2001.
[3] Nature Med. 7, 108. Mabley, G.J., et al. 2001. Inflamm. Res. 50, 561.
分子式
C17H17N3O2.HCl |
分子量
331.8 |
CAS号
344458-15-7 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
100 mM |
Water
100 mM |
Ethanol
<1 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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