Description | MDR-1339 is a blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation. |
In vitro | MDR-1339对一系列CYP同功酶没有明显的抑制作用,但对CYP2C8有轻微的抑制作用(IC50:31.4 μM)。MDR-1339(1.5-10 μM)可保护细胞免受Aβ诱导的毒性损伤。此外,MDR-1339(3.1-50 μM)还能剂量依赖性地阻止Aβ聚集体的形成,并解散Aβ纤维。 |
In vivo | MDR-1339(0.1-10 mg/kg,p.o.)在小鼠阿尔茨海默病模型中剂量依赖性地恢复被动回避反应(ED50:0.19 mg/kg)。MDR-1339(30和100 mg/kg,每日一次口服,持续8周)显著改善APP/PS1小鼠的自发性交替反应,并降低Aβ1-40与Aβ1-42水平。 |
Synonyms | DWK-1339 |
molecular weight | 326.39 |
Molecular formula | C20H22O4 |
CAS | 1018946-38-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 40 mg/mL (122.55 mM), Sonication is recommended. |
References | 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. |