Apabetalone (RVX-208)

For research use only.

Catalog No.S7295 Synonyms: RVX-000222

9 publications

Apabetalone (RVX-208) Chemical Structure

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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Selleck's Apabetalone (RVX-208) has been cited by 9 publications

3 Customer Reviews

  • 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.

    Effect of Bromodomain inhibitors on Ad infection. A549 cells were mock-treated (0.1% DMSO in culture medium) or treated with RVX-208 at 500 nM, PFI-1 at 500 nM, JQ1 at 300 nM, or with 300 nM (−)-JQ1, an inactive enantiomer of JQ1. The cells were then infected with Ad2 at 1 PFU/cell for 24 h. The compounds were left in the culture medium throughout the infection. Viral hexon and penton base (PB) protein was detected by immunoblotting analysis. GADPH expression was used as a loading control. The experiment was performed 3 times independently.

    Sci Rep, 2018, 8(1):11554. Apabetalone (RVX-208) purchased from Selleck.

  • Apabetalone increased cyclin T1 expression and induced CDK9 T-loop and RNAP II CTD phosphorylation in ACH2 cells in time-dependent manners.

    Acta Pharmacol Sin, 2018, doi:10.1038/s41401-018-0027-5. Apabetalone (RVX-208) purchased from Selleck.

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Biological Activity

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.
BD2 [1]
(Cell-free assay)
0.51 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 MXzGeY5kfGmxbjDhd5NigQ>? MYH+OlAh|ryP NHLWU4pFVVOR NXSyPVVYcW6mdXPld{BieG:DLVmgcXJPSSCjbnSg[IUhdm:4bzDzfY51cGW|aYOgc4Yh[XCxQT3JMi=> M4flVFIxPTF|NUm5
U2OS MYTGeY5kfGmxbjDhd5NigQ>? NYrlR3FEhjVizszN NGDEfYhlcXOybHHj[ZMhSkWWIIDyc5RmcW6|IH\yc40h[2i{b33heIlv M33ZTFI1OjR6M{e5

... Click to View More Cell Line Experimental Data

In vivo RVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways. [3]


Animal Research:


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  • Animal Models: Naïve adult male AGMs
  • Dosages: ~60 mg/kg
  • Administration: Oral gavage or intravenous administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC Na (1N HCl, PH 2.5-3.0)
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 370.4


CAS No. 1044870-39-4
Storage powder
in solvent
Synonyms RVX-000222
Smiles COC1=CC(=C2C(=O)NC(=NC2=C1)C3=CC(=C(OCCO)C(=C3)C)C)OC

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03160430 Not yet recruiting Drug: apabetalone|Drug: Placebos Kidney Failure Chronic Resverlogix Corp March 1 2020 Phase 1|Phase 2
NCT03228940 Not yet recruiting Drug: RVX000222 Fabry Disease Resverlogix Corp September 30 2019 Phase 1|Phase 2
NCT01863225 Terminated Drug: RVX000222|Drug: Rosuvastatin|Drug: Atorvastatin Dyslipidemia|Coronary Artery Disease Resverlogix Corp|South Australian Health and Medical Research Institute May 2013 Phase 2
NCT01728467 Completed Drug: RVX000222|Drug: Placebo RVX000222 Diabetes Resverlogix Corp|Baker IDI Heart and Diabetes Institute|Nucleus Network Ltd November 2012 Phase 2
NCT01067820 Completed Drug: RVX000222|Drug: Placebo RVX000222 Coronary Artery Disease Resverlogix Corp|The Cleveland Clinic September 2011 Phase 2
NCT01423188 Completed Drug: RVX000222|Drug: Placebo RVX000222 Coronary Artery Disease|Dyslipidemia Resverlogix Corp|The Cleveland Clinic August 2011 Phase 2

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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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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID