MDR-1339-DWK-1339-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMDR-1339Cat. No.: HY-14503CAS No.: 1018946-38-7Synonyms: DWK-1339分式: CHO分量: 326.39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(shù)據(jù)體外實驗 DMSO : 83.3 mg/mL (255.22 mM)*

2、 means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.0638 mL 15.3191 mL 30.6382 mL5 mM 0.6128 mL 3.0638 mL 6.1276 mL10 mM 0.3064 mL 1.5319 mL 3.0638 mL請根據(jù)產(chǎn)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 MDR-1339 (DWK-1339)種可服的，透過腦屏障的 A 聚集抑制劑，可于阿爾

3、茲海默癥的研究。IC50 & Target Amyloid- 1體外研究MDR-1339 is an A-aggregation inhibitor, and shows no significant inhibition a panel of CYP isozymes, while1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEit slightly inhibits CYP2C8 (IC50, 31.4 M). MDR-1339 (3.1-50 M) dose-dependently blocks the formation ofA agg

4、regates, and disaggregates A fibrils. MDR-1339 (1.5-10 M) also protects cells from this A-inducedtoxicity 1.體內(nèi)研究 MDR-1339 (0.1-10 mg/kg, p.o.) dose-dependently restores the passive avoidance responses in mice modelsof Alzheimers disease (AD), with an ED50 of 0.19 mg/kg. MDR-1339 (30 and 100 mg/kg, p

5、.o. daily for 8weeks) significantly improves spontaneous alternation, and reduces the A1-40 and A1-42 levels inAPP/PS1 mice 1.PROTOCOLCell Assay 1 HT22 cells, a murine cell line of hippocampal origin, are grown in Dulbeccos modified Eagles medium(DMEM) containing 10% fetal bovine serum and 5% penici

6、llin/streptomycin. At the outset, 90% confluentcells are dissociated and plated at 5 103 cells/well in a 96-well plate. When the cells are attached to theplate, the medium is replaced with plain DMEM. The cells are treated with MDR-1339. One hour after MDR-1339 treatment, 4 L of pre-diluted 25 M A42

7、 is added to the media, and the cells are further incubated for18 h. For the determination of cell viability, 15 L of 5 mg/mL MTT is added to each well and incubated for 3h. The formazan that formed is dissolved in DMSO, and the absorbance is measured at 570-630 nm using aplate reader 1.MCE has not

8、independently confirmed the accuracy of these methods. They are for reference only.Animal For this study, a total of 24 (n = 8 for each group) APP/PS1 B6C3-Tg (APPswe, PSEN1dE9) 85Dbo/J TgAdministration 1 mice are utilized. The mice are housed in a controlled environment under standard room temperat

9、ure,relative humidity and a 12 h light/dark cycle with free access to food and water. APP/PS1 treated groups areorally administered with MDR-1339 at a dose of 30 or 100 mg/kg body weight once daily. MDR-1339treatment is at the age of 29 weeks, and the treatment is conducted for 8 weeks 1.MCE has not

10、 independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ha HJ, et al. Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a -Amyloid Aggregation Inhibitor for thePotential Treatment of Alzheimers Disease. J Med Chem. 2018 Jan 11;61(1):396-402.McePdfHeightCaution: Product has not been fully vali