| Identification | Back Directory | [Name]
Piperazine, 1-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]-4-(2-pyridinyl)- | [CAS]
876685-78-8 | [Synonyms]
Piperazine, 1-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]-4-(2-pyridinyl)- | [Molecular Formula]
C18H19N5O | [MOL File]
876685-78-8.mol | [Molecular Weight]
321.38 |
| Chemical Properties | Back Directory | [Boiling point ]
514.9±60.0 °C(predicted) | [density ]
1.241±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
8.43±0.19(predicted) |
| Hazard Information | Back Directory | [Uses]
AChE-IN-63 (Compound 5AD) is a selective inhibitor of hAChE (IC50=0.103 μM). AChE-IN-63 also inhibits hBChE and hBACE-1 (IC50= 10 μM (hBChE); 1.342 μM (hBACE-1)). AChE-IN-63 inhibits Aβ aggregation, preventing the formation and deposition of Aβ1-42. AChE-IN-63 can effectively penetrate the blood-brain barrier and is orally effective. It is primarily used in Alzheimer's disease research[1]. | [in vivo]
AChE-IN-63 (p.o.; 100 mg/kg; single dose) exhibits no toxicity or abnormal reactions in Swiss albino mice[1].
AChE-IN-63 (p.o.; 5-20 mg/kg; single dose) improves learning and memory in cognitive dysfunction mice in the Scopolamine (HY-N0296) Y-Maze Model and demonstrates good antioxidant properties[1].
| Animal Model: | Scopolamine Y-Maze Model [1] | | Dosage: | 5; 10 ;20 mg/kg | | Administration: | p.o.; single dose | | Result: | Showed significant improvement in spontaneous alternation behavior.
Reduced AChE and MDA levels and increased CAT levels. |
| [IC 50]
hAChE: 0.103 μM (IC50); hBCHE: 10 μM (IC50) | [References]
[1] Singh A, et al. Structure-Guided Design, Synthesis, and Biological Evaluation of Peripheral Anionic Site Selective and Brain Permeable Novel Oxadiazole-Piperazine Conjugates against Alzheimer's Disease with Antioxidant Potential. ACS Omega. 2024 Apr 11;9(16):18169-18182. DOI:10.1021/acsomega.3c10276 |
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