| Name | Apabetalone |
| Description | Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease. |
| Cell Research | RVX-208 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 μM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 μg/mL for 3 hours[2]. |
| In vitro | In AGMs, RVX-208 significantly increases serum apoA-I and HDL-C levels and enhances cholesterol efflux through various pathways. |
| In vivo | In vitro studies have demonstrated that RVX-208 activates the expression of the apolipoprotein AI gene, leading to an increase in apoA-I and HDL-C levels. Additionally, RVX-208 inhibits BET bromodomain proteins, exhibiting a preferential binding to the second bromodomain of BET proteins. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (161.99 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | RVX-000222 | Inhibitor | Epigenetic Reader Domain | RVX 000222 | RVX208 | Human immunodeficiency virus | inhibit | RVX 208 | HIV | Apabetalone |
| Inhibitors Related | Stavudine | Emtricitabine | Lamivudine |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
