Molecular Formula | C20H22N2O5 |
Molar Mass | 370.4 |
Density | 1.28±0.1 g/cm3(Predicted) |
Boling Point | 594.2±60.0 °C(Predicted) |
Appearance | Form solid, color White |
pKa | 14.21±0.10(Predicted) |
Storage Condition | -20°C (des.) |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
Physical and Chemical Properties | Bioactive RVX-208 is an effective BET bromodomain inhibitor, acting on BD2 with IC50 of 0.510 μM, which is 170 times more selective than acting on BD1. Phase 2. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.7 ml | 13.499 ml | 26.998 ml |
5 mM | 0.54 ml | 2.7 ml | 5.4 ml |
10 mM | 0.27 ml | 1.35 ml | 2.7 ml |
5 mM | 0.054 ml | 0.27 ml | 0.54 ml |
in vitro studies
As a BET bromine domain protein inhibitor, the RVX-208 preferentially binds to the second bromine domain protein based on the BET protein. RVX-208, as an agonist of apolipoprotein (APO) AI gene expression, increased apoA-I and HDL-C in vitro.
In vivo studies
RVX-208 significantly increased serum apoA-I and HDL-C in AGMs, and increased cholesterol outflow through different routes.
Features
The first new drug BD2 selective BET bromine domain protein inhibitor was tested in a phase II clinical trial for the treatment of coronary syndrome and atherosclerosis.