H3R antagonist 4
H3R antagonist 4
SKU:QM-0092323
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Product Details
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Description
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 Aβ1-42 induced by itself and Cu2+ (95.48% and 88.63%), and degraded the Aβ1-42 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 Aβ1-42 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 Alzheimer's disease induced by scopolamine.
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Molecular Formula
C30H36N2O9
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Molecular Weight
568.61
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Smiles
CC(C)[C@@H](C(O)=O)NC(OC1=CC2=C(C(O)=C1O)C(C=C(C3=CC=C(OCCCN4CCCCCC4)C=C3)O2)=O)=O
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Target
Apoptosis; Cholinesterase (ChE) ; Ferroptosis; Histamine Receptor; Tau Protein
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Isoform
AChE; BChE
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Shipping Conditions
Room temperature
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H3R antagonist 4
H3R antagonist 4 is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.