1018946-38-7

DWK-1339 is an inhibitor of amyloid-β (Aβ) aggregation. 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 μM. DWK-1339 (10 μM) 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.

DWK-1339, is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer''s disease.

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[1] HEE-JIN HA. Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a β-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer’s Disease[J]. Journal of Medicinal Chemistry, 2017, 61 1: 396-402. DOI: 10.1021/acs.jmedchem.7b00844