生物活性 | |||
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描述 | DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor. DAAO is a flavoenzyme that degrades D-amino acids through the process of oxidative deamination[1]. DAAO treatment significantly increased RGCs (retinal ganglion cells) survival in the glaucomatous eyes. DAAO treatment induced ERK-1/2 MAP kinase phosphorylation and its upstream regulator, p-MEK increased in the COH (chronic intraocular hypertension) model[2]. Single intravenous injection of the specific and potent DAAO inhibitor Compound SUN reduced the cerebral DAAO enzymic activity and attenuated neuronal infarction and neurobehavioural deficits with optimal improvement apparent immediately after the middle cerebral artery occlusion (MCAO) procedure. The neuroprotective effect was dose dependent, with ED50 values of 3.9-4.5 mg/kg. Intracerebroventricular injection of the DAAO gene silencer siRNA/DAAO significantly reduced cerebral DAAO expression and attenuated MCAO-induced neuronal infarction and behavioural deficits[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.57mL 1.31mL 0.66mL |
32.87mL 6.57mL 3.29mL |
65.73mL 13.15mL 6.57mL |
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