 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1044870-39-4 |
| Molecular formula(MF) | C20H22N2O5 |
| Molecular Weight(MW): | 370.4 |
| Alias |
| In vitro | DMSO | 74 mg/mL (199.78 mM) |
|---|---|---|
| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL | |
| In vivo | 0.5% CMC Na (1N HCl, PH 2.5-3.0) | 8mg/mL |
| Description | RVX-208 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. | |||||||||||||||||||||||
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| Features | First-in-class BD2-selective inhibitor of BET bromodomain and has been tested in Phase II clinical trials for treatment of coronary syndromes and atherosclerosis. | |||||||||||||||||||||||
| Targets |
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| In vitro |
As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins. [1] RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro. [2] [3] |
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| Cell Data |
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| In vivo | RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3] |