Bioactivity | 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]. | ||||||||||||
Target | Kd: 5-10 μM (apoE3 and apoE4) | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | EZ-482 | ||||||||||||
CAS | 1016456-76-0 | ||||||||||||
Formula | C23H19ClN4O5S | ||||||||||||
Molar Mass | 498.94 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Tridib Mondal, et al. ApoE: In Vitro Studies of a Small Molecule Effector. Biochemistry. 2016 May 10;55(18):2613-21. |