Description
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
Formal name: trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
Synonyms:
Molecular weight: 638.7
CAS: 1186486-62-3
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Cardiovascular System|Lipids & Lipoproteins|Storage & Transport||Research Area|Lipid Biochemistry|Sterol Lipids
