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EZ-482

Names

[ CAS No. ]:
1016456-76-0

[ Name ]:
EZ-482

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

Kd: 5-10 μM (apoE3 and apoE4)[1]


[In Vitro]

EZ-482 binds to sites on apoE in the C-terminal domain encompassing residues 229-243 and 258-265[1]. EZ-482 (0.5, 1, 5, 10 μM; 1 hour) blocks heparin binding in a concentration-dependent manner[1].

[References]

[1]. Tridib Mondal, et al. ApoE: In Vitro Studies of a Small Molecule Effector. Biochemistry. 2016 May 10;55(18):2613-21.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H19ClN4O5S

[ Molecular Weight ]:
498.94


Related Compounds