| Identification | Back Directory | [Name]
Pyridine, 5-[5-[3-[[1-[(3-fluorophenyl)methyl]-4-piperidinyl]methoxy]phenyl]-1,2,4-oxadiazol-3-yl]-2-methyl- | [CAS]
2417117-84-9 | [Synonyms]
AChE/Nrf2 modulator 1
Pyridine, 5-[5-[3-[[1-[(3-fluorophenyl)methyl]-4-piperidinyl]methoxy]phenyl]-1,2,4-oxadiazol-3-yl]-2-methyl- | [Molecular Formula]
C27H27FN4O2 | [MOL File]
2417117-84-9.mol | [Molecular Weight]
458.53 |
| Hazard Information | Back Directory | [Uses]
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease[1]. | [in vivo]
AChE/Nrf2 modulator 1 (Compound 15a) (oral; 10 mg/kg; for 10 consecutive days) effectively shortens the latency time and escape distance to the target, increased the arrival times, and simplified the tracks in Morris water maze test induced by scopolamine and Aβ1-42[1].
AChE/Nrf2 modulator 1 (10, 20 mg/kg; intragastric administration) significantly reduces the levels of proinflammatory factors in the mice model brains[1]. | Animal Model: | ICR mice[1] | | Dosage: | 10, 20 mg/kg | | Administration: | Intragastric administration; oral; for 10 consecutive days | | Result: | Significantly reduced the latency time to target and simplified the traveled distance and exhibited a good effect on ameliorating ethological changes and spatial memory impairment by rescuing cholinergic function
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Showed an obvious reduction of pro-inflammation factors level and significantly increased the content of TGF-β1.
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| [References]
[1] Yuanyuan Wang, et al. Design, synthesis and evaluation of fused hybrids with acetylcholinesterase inhibiting and Nrf2 activating functions for Alzheimer's disease. Eur J Med Chem. 2022 Dec 15;244:114806. DOI:10.1016/j.ejmech.2022.114806 |
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