生物活性 | |||
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描述 | DR2313 is a potent, selective, competitive and brain-penetrating PARP inhibitor with IC50 values of 0.20 μM for PARP-1 and 0.24 μM for PARP-2. DR2313 is neuroprotective against ischaemic injury in vitro and in vivo[1][2].In the concentration range of 0.016-16.4 μM, DR2313 can inhibit the poly(ADP-ribosyl)ation reaction in rat brain nuclear extract for 30 minutes, with a Ki of 0.23 μM. In the concentration range of 1-100 μM, DR2313 showed a weak inhibitory effect on mono(ADP-ribosyl)ation in a concentration-dependent manner for 10 minutes, with an IC50 value of 59 μM. DR2313 reduces hydrogen peroxide (500 μM; 4 hours) or glutamate (1 mM; 30 minutes)-induced poly(ADP-ribose) and cell death in the concentration range of 0.1-30 μM and 30 minutes of pretreatment[1] . |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
5.49mL 1.10mL 0.55mL |
27.44mL 5.49mL 2.74mL |
54.87mL 10.97mL 5.49mL |
参考文献 |
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