| Description | LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin. |
| In vitro | 在APPV717F小鼠Aβ病理模型中,LY2811376（10/30/100 mg/kg）使Aβ、sAPPβ和C99出现剂量依赖性的显著减少,这些是APP被BACE1蛋白水解后最接近的分解产物.在比格犬体内,LY2811376（5 mg/kg）使血浆中的Aβ1-x减少,给药4-12 h后最大下降85%. |
| In vivo | LY2811376浓度依赖性降低APP过表达HEK293细胞中Aβ的分泌。LY2811376浓度依赖性抑制hBACE1,包括小分子合成肽（IC50：239 nM）和较大的嵌合蛋白底物（IC50：249 nM）。在PDAPP转基因小鼠的神经元原代培养物中,LY2811376抑制Aβ分泌（EC50：100 nM）。 |
| Cell experiments | The cytotoxicity in the HEK293Swe cell model is assessed using a CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. (Only for Reference) |
| Target activity | BACE1:239 nM-249 nM, β-Amyloid:300 nM(EC50) |
| molecular weight | 320.36 |
| Molecular formula | C15H14F2N4S |
| CAS | 1194044-20-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 13 mg/mL (40.6 mM) Ethanol: 60 mg/mL (187.3 mM) |
| References | 1. May P, et al. J Neurosci, 2011, 31(46), 16507-16516. 2. Yang HC, et al. J Neurochem, 2004, 91(6), 1249-1259. |