Evacetrapib

Evacetrapib

CAT N°: 23670
Price:

From 122.00 103.70

Evacetrapib is a benzazepine inhibitor of cholesteryl ester transfer protein (CETP; IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively).{41797} It is selective for CETP over a panel of cell surface and nuclear receptors with no significant inhibition at 1 µM. Evacetrapib (1-10 µM) reduces expression of the serine protease proprotein convertase subtilisin kexin 9 (PCSK9) and the LDL receptor (LDLR) in HepG2 cells in a dose-dependent manner with no effect on cell viability.{41798} It also reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner. Oral administration of evacetrapib (30 mg/kg) inhibits CETP activity by 98.5, 98.6, and 18.4% after four, eight, and 24 hours, respectively, in serum from transgenic mice expressing human CETP and ApoA1.{41797} Evacetrapib increases HDL cholesterol levels in CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours following administration of a 30 mg/kg dose.

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