化合物Edonerpic maleate T4422

Product Introduction
Bioactivity


英文名: Edonerpic maleate

描述: Edonerpic maleate (T-817 maleate) 是新神经营养剂，对淀粉样蛋白 β 肽具有抑制作用。

细胞实验: A cortical neuron/glia coculture is prepared. Edonerpic maleate (T-817MA) is added to the cocultures at concentrations of 0 (control), 0.01, 0.1, and 1 μM, and the cells are subsequently incubated for 5 min or 24 h. H2O2 is then added to the coculture at a concentration of 100 μM, and the cells are incubated for another 24 h. For the normal group, the preparations are maintained in the medium with neither Edonerpic maleate nor H2O2. Neuronal cell viability is quantified by measuring the Monoclonal anti-microtubule-associated protein 2 (MAP2) immunoreactivity

动物实验: Edonerpic maleate (T-817MA) (high-dose: 8.4 mg/kg and low-dose: 0.84 mg/kg) and donepezil (0.5 mg/kg) are dissolved in distilled water in a volume of 5 mL/kg.Wistar rats (7 weeks, n=47) are used in this study. All rats are given food and water ad libitum in a clear cage and handled on three consecutive days before start of the experiments. The housing area is provided a temperature-controlled environment under a 12/12 h light cycle. These rats are divided into five groups: vehicle (n=11), Aβ infusion control (n=10), Aβ infusion+high-dose Edonerpic maleate (T-817MA) (8.4 mg/kg) (n=11), Aβ infusion+low-dose Edonerpic maleate (0.84 mg/kg) (n=9) and Aβ infusion+donepezil (0.5 mg/kg) (n=7)

体外活性: Edonerpic maleate (T-817MA) treatment preserves the cortical neurons in the presence of Aβ(1-42). Twenty-four hours of pretreatment, followed by the continuous presence of Edonerpic maleate, prevents oxidative stress-induced neuronal death at 0.1 and 1 μM. Edonerpic maleate almost completely prevents GSH reduction at 0.1 and 1 μM. Hippocampal slices with 1 μM Edonerpic maleate treatment generate more and much longer neurites compared to controls. Edonerpic maleate significantly increases the neurite length at 0.1 and 1 μM.

体内活性: The post hoc test indicates that the average density of PSA-positive cells is significantly larger in the vehicle and Aβ infusion+high-dose Edonerpic maleate (T-817MA) groups than that in the Aβ infusion control group (P<0.01). The results indicate that the vehicle and Aβ infusion+high-dose Edonerpic maleate groups display efficient learning in the place learning task (PLT), while these two groups also display vigorous neurogenesis. Treatment with Edonerpic maleate and donepezil does not increase the mean density of normal granule cells; there are no significant differences in the mean granule cell density among the Aβ infusion control, Aβ infusion+high-dose Edonerpic maleate, Aβ infusion+low-dose Edonerpic maleate and Aβ infusion+donepezil groups.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 155 mg/mL(380 mM)


关键字: Inhibitor | β-amyloid peptide | T 817 Maleate | Abeta | Amyloid-β | Edonerpic Maleate | T 817 | Edonerpic | T817 | Edonerpic maleate | T-817 | inhibit | T817 Maleate | T-817 Maleate

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