| Bioactivity | AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD)[1]. |
| Invitro | AChE/BACE1/GSK3β-IN-1 shows effective inhibition for AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively[1].AChE/BACE1/GSK3β-IN-1 can pass through BBB[1]. |
| In Vivo | AChE/BACE1/GSK3β-IN-1 (oral, 200 and 400 mg/kg, single) shows no acute toxicity and good safety profile in C57B6/J Mice[1].AChE/BACE1/GSK3β-IN-1 (p.o., 100 mg/kg; i.v., 10 mg/kg)has good PK profiles[1].AChE/BACE1/GSK3β-IN-1 (gavage, 2.5 mg/kg, 5 mg/kg and 10mg/kg, for 7 consecutive days) can ameliorate the impaired learning and memory in Aβ-induced AD mice[1].AChE/BACE1/GSK3β-IN-1 inhibits the expression of ADAM17 in the cortex and significantly decreases the expressions of ADAM17 and BACE1 in AD mice[1]. Animal Model: |
| Name | AChE/BACE1/GSK3β-IN-1 |
| Formula | C26H27FN2O4 |
| Molar Mass | 450.50 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Nan Wang, et al. Design, Synthesis, and Biological Evaluation of Notopterol Derivatives as Triple Inhibitors of AChE/BACE1/GSK3β for the Treatment of Alzheimer’s Disease. ACS Omega 2022, 7, 36, 32131–32152. Publication Date:August 30, 2022. |