For research use only.
Catalog No.S7295 Synonyms: RVX-000222
CAS No. 1044870-39-4
Apabetalone (RVX-208, RVX-000222) 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.
Selleck's Apabetalone (RVX-208) has been cited by 14 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.
Purity & Quality Control
Choose Selective Epigenetic Reader Domain Inhibitors
|Description||Apabetalone (RVX-208, RVX-000222) 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 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03160430||Unknown status||Drug: apabetalone|Drug: Placebos||Kidney Failure Chronic||Resverlogix Corp||March 1 2020||Phase 1|Phase 2|
|NCT03228940||Unknown status||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 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|
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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