H3R antagonist 4
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 (HY-N0296) [1] .
Product Specifications
UNSPSC
12352005
Target
Apoptosis; Cholinesterase (ChE) ; Ferroptosis; Histamine Receptor; Tau Protein
Type
Reference compound
Related Pathways
Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling
Applications
Neuroscience-Neurodegeneration
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/h3r-antagonist-4.html
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
Molecular Formula
C30H36N2O9
Molecular Weight
568.61
References & Citations
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-162812/H3R-antagonist-4-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-162812/
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
AChE; BChE
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