MDR-1339

• CAT Number: I020252
• CAS Number: 1018946-38-7
• Molecular Formula: C20H22O4
• Molecular Weight: 326.39
• Purity: ≥95%
• Synonyms: 2-(3,4-dimethoxyphenyl)-5-(3-methoxypropyl)-1-benzofuran
• InChI: InChI=1S/C20H22O4/c1-21-10-4-5-14-6-8-17-16(11-14)13-19(24-17)15-7-9-18(22-2)20(12-15)23-3/h6-9,11-13H,4-5,10H2,1-3H3
• InChIKey: CUEPJIGXQLIOIK-UHFFFAOYSA-N
• SMILES: COCCCC1=CC2=C(C=C1)OC(=C2)C3=CC(=C(C=C3)OC)OC

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

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.
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