| Description | ELN318463 racemate (ELN 318463 racemate) is the racemate of ELN318463 which is an amyloid precursor protein (APP) selective γ-secretase inhibitor. |
| In vitro | ELN318463对含有PS1和PS2的γ-分泌酶表现出不同的抑制作用，其对PS1和PS2的EC50分别为12nM和656nM[1]。 |
| In vivo | 在FVB小鼠脑中，ELN318463（30 mg/kg）的脑部浓度为0.754 μM，而在PDAPP小鼠脑中为0.69 μM。当剂量增加至100 mg/kg 时，ELN318463在FVB小鼠脑中的浓度上升至2.7 μM，在PDAPP小鼠脑中为1.87 μM[1]。 |
| Synonyms | ELN318463 (racemate), ELN 318463 racemate |
| molecular weight | 471.8 |
| Molecular formula | C19H20BrClN2O3S |
| CAS | 851599-82-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (105.98 mM) |
| References | 1. Zhao B, et al. Identification of gamma-secretase inhibitor potency determinants on presenilin. J Biol Chem. 2008 Feb 1;283(5):2927-38. 2. Basi GS, et al. Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease. Alzheimers Res Ther. 2010 Dec 29;2(6):36. |