LXRβ agonist CL2-57 is a non-lipogenic ABCA1 inducer and an LXRβ-selective agonist (EC50=1.3 uM) and PPAR/RXR antagonist.
CL2-57 enhances ABCA1-linked luciferase activity in HepG2 liver cells (Emax=250%; EC50=1.8 uM).
CL2-57 selectively induces ABCA1 and lessens inflammation in vitro, CL2-57 dose-dependently increased cholesterol efflux from macrophages to apoA1, the primary acceptor of cholesterol from ABCA1 in vivo.
CL2-57 (10 mg/kg oral gavage) enhances glucose tolerance and insulin sensitivity in mice fed a high-fat diet (HFD).
CL2-57 reduces HFD-induced adiposity and alterations in liver gene expression, also reduces gluconeogenic metabolite, broadly attenuated pro-inflammatory cytokines, enzymes, and metabolites in HFD mice.
