TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRalpha and LXRbeta, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRalpha/beta transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders[1].
Molekulargewicht:
739.12
Formel:
C38H22ClF3N4O5S
Target-Kategorie:
LXR
Anwendungsbeschreibung:
MCE Product type: Reference compound
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