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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEdonerpic maleateCat. No.: HY-17631ACAS No.: 519187-97-4Synonyms: T-817 maleate; T-817MA分式: CHNOS分量: 407.48作靶點: Amyloid-作通路: Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO
2、: 155 mg/mL (380.39 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4541 mL 12.2705 mL 24.5411 mL5 mM 0.4908 mL 2.4541 mL 4.9082 mL10 mM 0.2454 mL 1.2271 mL 2.4541 mL請根據產品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Edonerpic maleate種新的神經營養(yǎng)劑,其可以抑
3、制淀粉樣蛋 肽 (A)。IC50 & Target amyloid- peptides 1體外研究Edonerpic maleate (T-817MA) treatment preserves the cortical neurons in the presence of A(1-42). Twenty-four hours of pretreatment, followed by the continuous presence of Edonerpic maleate, prevents oxidative1/2 Master of Small Molecules 您邊的抑制劑師www.Me
4、dChemEstress-induced neuronal death at 0.1 and 1 M. Edonerpic maleate almost completely prevents GSHreduction at 0.1 and 1 M. Hippocampal slices with 1 M Edonerpic maleate treatment generate more andmuch longer neurites than control slices. Edonerpic maleate significantly increases the neurite lengt
5、h at 0.1and 1 M 1.體內研究 The post hoc test indicates that the mean density of PSA-positive cells is significantly larger in the vehicleand A infusion+high-dose Edonerpic maleate (T-817MA) groups than that in the A infusion control group(P 2.PROTOCOLCell Assay 1 A cortical neuron/glia coculture is prep
6、ared. Edonerpic maleate (T-817MA) is added to the cocultures atconcentrations of 0 (control), 0.01, 0.1, and 1 M, and the cells are subsequently incubated for 5 min or 24 h.H2O2 is then added to the coculture at a concentration of 100 M, and the cells are incubated for another 24h. For the normal gr
7、oup, the preparations are maintained in the medium with neither Edonerpic maleate norH2O2. Neuronal cell viability is quantified by measuring the Monoclonal anti-microtubule-associated protein 2(MAP2) immunoreactivity 1.MCE has not independently confirmed the accuracy of these methods. They are for
8、reference only.Animal Wistar rats (7 weeks, n=47) are used in this study. All rats are given food and water ad libitum in a clear cageAdministration 2 and handled on three consecutive days before start of the experiments. The housing area is provided atemperature-controlled environment under a 12/12
9、 h light cycle. These rats are divided into five groups:vehicle (n=11), A infusion control (n=10), A infusion+high-dose Edonerpic maleate (T-817MA) (8.4 mg/kg)(n=11), A infusion+low-dose Edonerpic maleate (0.84 mg/kg) (n=9) and A infusion+donepezil (0.5 mg/kg)(n=7) 2.MCE has not independently confir
10、med the accuracy of these methods. They are for reference only.REFERENCES1. Hirata K, et al. A novel neurotrophic agent, T-817MA 1-3-2-(1-benzothiophen-5-yl) ethoxy propyl-3-azetidinol maleate, attenuatesamyloid-beta-induced neurotoxicity and promotes neurite outgrowth in rat cultured central nervou
11、s system neurons. J Pharmacol Exp Ther.2005 Jul;314(1):252-9.2. Kimura T, et al. T-817MA, a neurotrophic agent, ameliorates the deficits in adult neurogenesis and spatial memory in rats infused i.c.v.with amyloid-beta peptide. Br J Pharmacol. 2009 Jun;157(3):451-63.McePdfHeightCaution: Product has not be
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