LXRbeta ligand 1 is a LXR beta ligand-binding domain agonist, with an EC50 of 57 µM and a Ki of 28 µM against human LXR beta. LXRbeta ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation, its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a pi-pi stacking interaction with Phe329. LXRbeta ligand 1 serves as a structural unit for the development of LXRbeta modulators[1].
Molekulargewicht:
248.32
Reinheit:
99.95
CAS Nummer:
[171049-41-5]
Formel:
C14H20N2O2
Target-Kategorie:
LXR
Anwendungsbeschreibung:
MCE Product type: Reference compound
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