Cat No:LP000354
Product Name:RVX-208;Apabetalone;RVX000222
CAS#1044870-39-4
Molecular Formula:C20H22N2O5
Molecular Weight:370.40
RVX-208 competes with binding of an acetylated histone peptide to tandem BD1 BD2 protein constructs of the four BET proteins, with IC50s between 0.5 and 1.8 µM. RVX-208 increases the production of ApoA-I in hepatocytes in vitro, which results in increased high density lipoprotein cholesterol (HDL-C). RVX-208 selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. RVX-208 increases Apolipoprotein A-I (ApoA-I) production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. RVX-208 increases ApoA-I expression in liver cells.
