H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 µM (eeAChE), 9.73 µM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Abeta1-42 induced by itself and Cu2+ (95.48% and 88.63%) , and degraded the Abeta1-42 fibrils induced by itself and Cu2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu2+, Zn2+, Al3+, and Fe2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Abeta1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimers disease induced by scopolamine (HY-N0296) [1] .
Molekulargewicht:
568.61
Formel:
C30H36N2O9
Target-Kategorie:
Apoptosis,Cholinesterase (ChE),Ferroptosis,Histamine Receptor,Tau Protein
Anwendungsbeschreibung:
MCE Product type: Reference compound
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