| Bioactivity | AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD)[1]. |
| Target | IC50: 0.053 μM (hAChE); 0.088 μM (eeAChE) and 7.5μM (eqBuChE) |
| Invitro | AChE-IN-24 (compound 4c2) has good hAChE inhibitory activity with IC50values of 0.053 μM but owns little inhibition to hBuChE[1].AChE-IN-2 has inhibitory activity for electric eel acetylcholinesterase (eeAChE) and equine serum butyrylcholinesterase (eqBuChE) with IC50values of 0.088 μM and 7.5μM, respectively[1].AChE-IN-24 (0-0.2 μM) can cross the BBB comfortably by means of passive diffusion[1].AChE-IN-2 (0-40 μM) triggers the translocation of Nrf2 to the nucleus, thereby expediting the binding of Nrf2 to the ARE for the transcription process[1].AChE-IN-2 (7 μM) significantly induces the expression of antioxidant-related enzymes by activating Nrf2 in BV-2 cells[1].AChE-IN-2 (1, 3, 7 μM) protects cells from H2O2-induced damage and inhibits ROS accumulation[1].AChE-IN-2 (1, 3, 7 μM) attenuates inflammatory responses[1]. Cell Viability Assay[1] Cell Line: |
| In Vivo | AChE-IN-24 (compound 4c2) (oral; 0, 625, 1250, and 2500 mg/kg) is well tolerated and no toxicity in KM mice[1].AChE-IN-24 (7.5 mg/kg, 15 mg/kg and 30mg/kg; once) ameliorates cognitive deficit induced by Scopolamine, suggesting a practicable therapeutic effect on AD[1]. Animal Model: |
| Name | AChE-IN-24 |
| Formula | C22H30N2O4S2 |
| Molar Mass | 450.61 |
| 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]. Jie Guo, et al. A multi-target directed ligands strategy for the treatment of Alzheimer's disease: Dimethyl fumarate plus Tranilast modified Dithiocarbate as AChE inhibitor and Nrf2 activator. Eur J Med Chem. 2022 Aug 11;242:114630. |