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Introduction of 1016456-76-0 :
EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas. IC50 & Target: Kd: 5-10 μM (apoE3 and apoE4)In Vitro: EZ-482 binds to sites on apoE in the C-terminal domain encompassing residues 229-243 and 258-265. EZ-482 (0.5, 1, 5, 10 μM; 1 hour) blocks heparin binding in a concentration-dependent manner.