| Bioactivity | MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease. | ||||||||||||
| Target | Amyloid-β | ||||||||||||
| Invitro | 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). MDR-1339 (3.1-50 μM) dose-dependently blocks the formation of Aβ aggregates, and disaggregates Aβ fibrils. MDR-1339 (1.5-10 μM) also protects cells from this Aβ-induced toxicity[1]. | ||||||||||||
| In Vivo | MDR-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. MDR-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]. | ||||||||||||
| Name | MDR-1339 | ||||||||||||
| CAS | 1018946-38-7 | ||||||||||||
| Formula | C20H22O4 | ||||||||||||
| Molar Mass | 326.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |