A benzazepine-based inhibitor of CETP (IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively); selective for CETP over a panel of cell surface and nuclear receptors at 1 μM; reduces expression of PCSK9 and LDLR in HepG2 cells in a dose-dependent manner; reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner; inhibits CETP activity by 98.5, 98.6, and 18.4% at four, eight, and 24 h, respectively, in CETP/ApoA1 transgenic mice at 30 mg/kg; increases HDL cholesterol levels in serum from CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours after a 30 mg/kg dose