Description
InformationApabetalone (RVX-208) Apabetalone (RVX-208, RVX-000222) is a potent BET bromodomain inhibitor with IC50 of 0.510 µM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.In vitroAs a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro.In vivoRVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways.Cell Datacell lines:CV-1 cellsConcentrations:Incubation Time:Powder Purity:≥98%