DWK-1339 (MDR-1339)

An inhibitor of amyloid-β aggregation

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5mg

￥1787.00

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10mg

￥3050.00

2440.00

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25mg

￥6037.00

4830.00

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50mg

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100mg

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13680.00

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Background

DWK-1339 is an inhibitor of amyloid-β (Aβ) aggregation.¹ It inhibits aggregation of monomeric Aβ (1-42) (Aβ42) and induces disaggregation of Aβ42 fibrils in vitro when used at concentrations ranging from 3.1 to 50 ?M. DWK-1339 (10 ?M) reduces Aβ42-induced toxicity in HT-22 cells. In vivo, DWK-1339 (10 mg/kg) increases step-through latency in a passive avoidance test and increases spontaneous alteration in the Y-maze compared with vehicle control mice in a mouse model of Aβ42-induced acute Alzheimer's disease. It also decreases brain levels of Aβ42 and increases spontaneous alteration in the Y-maze in the APP/PS1 transgenic mouse model of Alzheimer's disease.

1.Ha, H., Kang, D.W., Kim, H.-M., et al.Discovery of an orally bioavailable benzofuran analogue that serves as a β-amyloid aggregation inhibitor for the potential treatment of Alzheimer's diseaseJ. Med. Chem.61(1)396-402(2018)

Protocol

Cell experiment:

HT22 cells, a murine cell line of hippocampal origin, are grown in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum and 5% penicillin/streptomycin. At the outset, 90% confluent cells are dissociated and plated at 5 × 103 cells/well in a 96-well plate. When the cells are attached to the plate, the medium is replaced with plain DMEM. The cells are treated with MDR-1339. One hour after MDR-1339 treatment, 4 μL of pre-diluted 25 μM Aβ42 is added to the media, and the cells are further incubated for 18 h. For the determination of cell viability, 15 μL of 5 mg/mL MTT is added to each well and incubated for 3 h. The formazan that formed is dissolved in DMSO, and the absorbance is measured at 570-630 nm using a plate reader[1].

Animal experiment:

For this study, a total of 24 (n = 8 for each group) APP/PS1 [B6C3-Tg (APPswe, PSEN1dE9) 85Dbo/J] Tg mice are utilized. The mice are housed in a controlled environment under standard room temperature, relative humidity and a 12 h light/dark cycle with free access to food and water. APP/PS1 treated groups are orally administered with MDR-1339 at a dose of 30 or 100 mg/kg body weight once daily. MDR-1339 treatment is at the age of 29 weeks, and the treatment is conducted for 8 weeks[1].

参考文献:

[1]. Ha HJ, et al. Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a β-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease. J Med Chem. 2018 Jan 11;61(1):396-402.