| Chemical Properties | Back Directory | [Boiling point ]
585.2±50.0 °C(predicted) | [density ]
1.201±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
13.57±0.43(predicted) |
| Hazard Information | Back Directory | [Uses]
S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model[1]. | [IC 50]
eqBCHE: 0.059 μM (IC50); hBCHE: 0.162 μM (IC50) | [References]
[1] Chen Y, et al., Discovery of 4-benzylpiperazinequinoline BChE inhibitor that suppresses neuroinflammation for the treatment of Alzheimer's disease. Eur J Med Chem. 2024 Jun 5;272:116463. DOI:10.1016/j.ejmech.2024.116463 |
|
|