RVX-028, also known as RVX-000222, is a potent BET bromodomain inhibitor. It preferentially binds to the second bromodomain on BET proteins. It also stimulates apolipoprotein (APO) AI gene expression, which increases apoA-I and HDL-C in vitro. In vivo, RVX-208 enhances cholesterol efflux via different pathways and significantly increases serum apoA-I and HDL-C in monkeys.

RVX-000222

≥98% by HPLC

RVX-208 has been shown to have an IC50 = 0.510 μM for BD2, which is ~170-fold selectivity over BD1.

Solubility in DMSO is 74 mg/ml. Solubility in water and ethanol is <1 mg/ml.

A crystalline solid

Store at or below -20°C for up to two years.

Useful as a BET Bromodomain inhibitor.

1. Bailey, D., et al., J Am Coll Cardiol. 2010;55(23):2580-2589.
2. Picaud, S., et al., Proc Natl Acad Sci U.S.A. 2013; 110(49):19754-19759.
3. McNeill, E. Curr Opin Investig Drugs. 2010;11(3):357-364.

Bromodomain

Inhibitor