apabetalone-rvx-208-rvx000222

Description: Apabetalone (also known as RVX-208, RVX000222) is a novel and potent inhibitor of BET (Bromodomain and Extra-Terminal) bromodomain (BD) with potential anti-inflammatory activity and the potential to be used in the treatment of cardiovascular diseases. It inhibits BET (BD2) with an IC50 of 0.510 uM in a cell-free assay, and shows about 170-fold higher selectivity for BD2 over BD1. RVX-208 is currently undergoing phase III clinical trials for reducing the relative risk (RR) of major adverse cardiac events (MACE) in patients with cardiovascular disease (CVD). It acts by binding to the acetyl-lysine binding pocket in a peptide-competitive way. In HepG2 cells, RVX-208 induced messenger ribonucleic acid and protein synthesis of apolipoprotein (apo)A-I.

References: Proc Natl Acad Sci U S A. 2013; 110(49):19754-9; Curr Opin Investig Drugs. 2010; 11(3):357-64.

RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone.

Chemical Name: 2-(4-(2-hydroxyethoxy)-3, 5-dimethylphenyl)-5, 7-dimethoxyquinazolin-4(3H)-one

InChi Key: NETXMUIMUZJUTB-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10, 23H, 5-6H2, 1-4H3, (H, 21, 22, 24)

SMILES Code: O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3