Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.

BD2:0.51 μM

In AGMs, RVX-208 significantly increases serum apoA-I and HDL-C levels and enhances cholesterol efflux through various pathways.

In vitro studies have demonstrated that RVX-208 activates the expression of the apolipoprotein AI gene, leading to an increase in apoA-I and HDL-C levels. Additionally, RVX-208 inhibits BET bromodomain proteins, exhibiting a preferential binding to the second bromodomain of BET proteins.

RVX-208 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 μM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 μg/mL for 3 hours[2].