DR 2313

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DR 2313 是聚（ADP-核糖）聚合酶的竞争性抑制剂（对于 PARP-1 和 PARP-2，IC50 分别为 0.20 和 0.24 μM）。

DR 2313 is a competitive inhibitor of poly(ADP-ribose) polymerase (IC50: 0.20 and 0.24 μM for PARP-1 and PARP-2 respectively). It also has neuroprotective.

DR2313 (0.016-16.4 μM; 30 min) inhibits poly(ADP-ribosyl)ation reaction in nuclear extracts of rat brain, with a Ki 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.

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. Animal Model:Male Wistar rats (220-300 g) with permanent MCA occlusions (pMCAos) and transient MCA occlusions (tMCAos)Dosage:3, 10 mg/kg Administration:I.v. bolus and i.v. infusion for 6 h beginning 5 min before the onset of ischemiaResult:Reduced the infarct volume in a dose-dependent manner in pMCAo and tMCAo model.

——

Cell Cycle/DNA Damage

PARP

PARP1|PARP2

——

——

284028-90-6

182.24

C8H10N2OS

>98% (HPLC)

DMSO:83.3mg/mL;H2O:9.1mg/mL

O=C(N=C(C)N1)C2=C1CCSC2

——

(-20℃)

With Ice Pack

≥ 2 years