MDR-1339 是口服有效Aβ聚集抑制剂,可透过血脑屏障的。MDR-1339可用于阿尔兹海默症的研究。
产品描述
MDR-1339 is a blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
体外活性
MDR-1339 shows no significant inhibition of a panel of CYP isozymes, while it slightly inhibits CYP2C8 (IC50: 31.4 μM). MDR-1339 (1.5-10 μM) protects cells from this Aβ-induced toxicity. MDR-1339 (3.1-50 μM) also dose-dependently blocks the formation of Aβ aggregates and disaggregates Aβ fibrils.
体内活性
MDR-1339 (0.1-10 mg/kg, p.o.) dose-dependently restores the passive avoidance responses in mice models of Alzheimer's disease (ED50: 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.
Cas No.
1018946-38-7
分子式
C20H22O4
分子量
326.39
别名
DWK-1339
储存和溶解度
DMSO:80 mg/mL (245.11 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years