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

BD2:0.51 μM

在AGMs中,RVX-208能够显著增加血清apoA-I和 HDL-C,同时通过多种途径增加胆固醇流出.

在体外实验中,RVX-208能够激活载脂蛋白AI基因表达,增加apoA-I 和 HDL-C。RVX-208能够抑制BET溴结构域蛋白,并且优先与BET蛋白质的第二溴结构域蛋白结合。

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].