产品描述:
δ-Secretase inhibitor 11 is an inhibitor of δ-secretase (IC50 = 0.7 µM), also known as asparagine endopeptidase (AEP) and legumain.{65769} It is selective for δ-secretase over cathepsin S, cathepsin L, caspase-3, and caspase-8 (IC50s = >200, >200, 31.86, and 86.71 µM, respectively). δ-Secretase inhibitor 11 inhibits δ-secretase in Pala B-lymphoblastoid cells (IC50 = 0.8 µM). It inhibits glucose-oxygen deprivation-induced cell death in primary mouse neurons when used at a concentration of 2 µM. In vivo, δ-secretase inhibitor 11 (10 mg/kg per day) inhibits brain δ-secretase in wild-type mice and transgenic mice expressing human tauP301S. It reduces the number of cortical and hippocampal tau N368-positive neurons, restores synaptic dysfunction, and improves spatial learning and memory in transgenic mice expressing human tauP301S. δ-Secretase inhibitor 11 (10 mg/kg) reduces hippocampal amyloid-β (Aβ) deposition and attenuates cognitive deficits in the 5XFAD transgenic mouse model of Alzheimer’s disease.