DWK-1339是一种可口服的，透过血脑屏障的Aβ聚集抑制剂，可用于阿尔兹海默症的研究。
CAS：1018946-38-7
分子式：C20H22O4
分子量：326.39
纯度：98%
存储：Store at -20°C

Background:

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

DWK-1339 (MDR-1339) is an Aβ-aggregation inhibitor, and shows no significant inhibition a panel of CYP isozymes, while it slightly inhibits CYP2C8 (IC50, 31.4 μM). DWK-1339 (3.1-50 μM) dose-dependently blocks the formation of Aβ aggregates, and disaggregates Aβ fibrils. DWK-1339 (1.5-10 μM) also protects cells from this Aβ-induced toxicity[1].

DWK-1339 (0.1-10 mg/kg, p.o.) dose-dependently restores the passive avoidance responses in mice models of Alzheimer’s disease (AD), with an ED50 of 0.19 mg/kg. DWK-1339 (30 and 100 mg/kg, p.o. daily for 8 weeks) significantly improves spontaneous alternation, and reduces the Aβ1-40 and Aβ1-42 levels in APP/PS1 mice[1].

[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.