Catalog No.S7295 Synonyms: RVX-000222
Molecular Weight(MW): 370.4
Apabetalone (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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Bromodomain 1 or 2 of BET family proteins is involved in 3T3-L1 adipogenesis. (A) LY294002, RVX208 and JQ1 were applied to differentiating 3T3-L1 from day 2 to day 6. Phenyl acetate (PA), known as a PPAR-γ agonist was used as a positive control. Cells were labeled with ORO (Bar=50nm). (B) Schematic representation of specificity of each chemical inhibitor for Bromodomain BD1 and 2 and quantitative analysis of ORO staining. The IDMR treatment without drugs (CTL) was used to define 100%. Data are reported as means ± sd (n=3); *** p<0.001 vs IDM control; ### p<0.001 vs IDMR control (-)-JQ1); +++ p<0.01 vs IDM of each condition; ns, non significant.
BBRC, 2016, 472(4):624-630.. Apabetalone (RVX-208) purchased from Selleck.
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|Description||Apabetalone (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.|
|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.|
As a BET bromodomain inhibitor, RVX-208 preferentially binds to the second bromodomain found on BET proteins.  RVX-208, as a stimulator of apolipoprotein (APO) AI gene expression, increases apoA-I and HDL-C in vitro.  
|In vivo||RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. |
|In vitro||DMSO||74 mg/mL (199.78 mM)|
|In vivo||Add solvents individually and in order:
0.5% CMC Na (1N HCl, PH 2.5-3.0)
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02586155||Recruiting||Diabetes Mellitus, Type 2|Coronary Artery Disease|Cardiovascular Diseases||Resverlogix Corp|PPD|ICON plc|Medidata Solutions||October 2015||Phase 3|
|NCT01863225||Terminated||Dyslipidemia|Coronary Artery Disease||Resverlogix Corp|South Australian Health and Medical Research Institute||May 2013||Phase 2|
|NCT01728467||Completed||Diabetes||Resverlogix Corp|Baker IDI Heart and Diabetes Institute|Nucleus Network Ltd||November 2012||Phase 2|
|NCT01067820||Completed||Coronary Artery Disease||Resverlogix Corp|The Cleveland Clinic||September 2011||Phase 2|
|NCT01423188||Completed||Coronary Artery Disease|Dyslipidemia||Resverlogix Corp|The Cleveland Clinic||August 2011||Phase 2|
|NCT01058018||Completed||Atherosclerosis|Coronary Artery Disease||Resverlogix Corp||December 2009||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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