| Identification | Back Directory | [Name]
Acetamide, 2-[(4-fluorophenyl)amino]-N-[4-[3-[2-[[4-(trifluoromethoxy)phenyl]amino]-4-pyridinyl]-1,2,4-oxadiazol-5-yl]phenyl]- | [CAS]
2745118-93-6 | [Synonyms]
BuChE-IN-2
Acetamide, 2-[(4-fluorophenyl)amino]-N-[4-[3-[2-[[4-(trifluoromethoxy)phenyl]amino]-4-pyridinyl]-1,2,4-oxadiazol-5-yl]phenyl]- | [Molecular Formula]
C28H20F4N6O3 | [MOL File]
2745118-93-6.mol | [Molecular Weight]
564.49 |
| Hazard Information | Back Directory | [Uses]
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease[1]. | [in vivo]
BuChE-IN-2 (40.96-100 mg/kg; i.g., single) shows LD50 of 75.372 mg/kg in mice[1].
BuChE-IN-2 (10 and 30 mg/kg; i.g., single) can remarkably improve the cognitive impairment in scopolamine-induced mouse models according to Morris water maze experiment[1]. | Animal Model: | Male C57BL mice (8-week-old, 18-23 g)[1] | | Dosage: | 100, 80, 64, 51.2, 40.96 mg/kg | | Administration: | i.g.; single | | Result: | The median Lethal Dose (LD50) of BuChE-IN-2 was 75.372 (62.383-101.673) mg/kg (95% confidence limit). |
| Animal Model: | Male C57BL mice (8-week-old, 18-23 g)[1] | | Dosage: | 30 mg/kg, 10 mg/kg | | Administration: | i.g., single | | Result: | BuChE-IN-2 could remarkably improve the cognitive impairment in scopolamine-induced mouse models according to Morris water maze experiment. |
| [References]
[1] Liu T, et al. Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. Eur J Med Chem. 2022;227:113973. DOI:10.1016/j.ejmech.2021.113973 |
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