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Apabetalone (RVX-208) is a first-in-class, small molecule that inhibits BET bromodomains. RVX-208 binds to the BET protein, it triggers a cascade of events leading to increased ApoA-I gene transcription and eventually production of the protein. RVX-208 increases apoA-I and HDL-C in vitro and in vivo. In AGMs, RVX-208 raises serum pre-beta(1)-LpA-I and alpha-LpA-I levels and enhances cholesterol efflux.
| Molecular Weight | 370.4 |
| Formula | C20H22N2O5 |
| CAS Number | 1044870-39-4 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Dragana Nikolic, et al. An evaluation of RVX-208 for the treatment of atherosclerosis
[3] Kevin G McLure, et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist
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