DR2313,284028-90-6

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DR2313

CAS No. : 284028-90-6

MCE 国际站：DR2313

产品活性：DR2313 是一种有效，选择性，竞争性的和可透过血脑屏障的 PARP 抑制剂，抑制 PARP-1 和 PARP-2 的 IC₅₀ 值分别为 0.20 μM 和 0.24 μM。DR2313 在体外和体内均表现出对缺血性损伤的神经保护作用。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：PARP

In Vitro: DR2313 (0.016-16.4 μM; 30 min) inhibits poly(ADP-ribosyl)ation reaction in nuclear extracts of rat brain, with a K_i of 0.23 μM.
DR2313 shows more powerful inhibition of the poly(ADP-ribosyl)ation in the nuclear extracts of the rat brain (IC₅₀=0.20 μM) than 3AB (35.4 μM), PND (0.56 μM), DIQ (2.96 μM), and DPQ (0.96 μM).
DR2313 (1-100 μM; 10 min) shows a weak inhibition of the mono(ADP-ribosyl)ation in a concentration-dependent manner (IC₅₀=59 μM).
DR2313 (0.1-30 μM; pretreated for 30 min) reduces hydrogen peroxide (500 μM; 4 h) or glutamate (1 mM; 30 min) induced excessive formation of poly(ADP-ribose) and cell death.

In Vivo: DR2313 (3-10 mg/kg i.v. bolus or infusion for 6 h) significantly reduces the cortical infarct volume in both permanent and transient focal ischemia models in rats.

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