Apabetalone (RVX-208)

Catalog No.S7295 Synonyms: RVX-000222

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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  • 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.
Targets
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 M3rFfWZ2dmO2aX;uJIF{e2G7 M2PWW543OCEQvF2= M4S5N2ROW09? NUT2SJBVcW6mdXPld{BieG:DLVmgcXJPSSCjbnSg[IUhdm:4bzDzfY51cGW|aYOgc4Yh[XCxQT3JMi=> NWe3U5NbOjB3MUO1PVk>
U2OS NWPWOpNlTnWwY4Tpc44h[XO|YYm= MUn+OUDPxE1? NYG0OWV6\Gm|cHzhZ4V{KEKHVDDwdo91\WmwczDmdo9uKGOqcn;tZZRqdg>? MV6yOFI1QDN5OR?=

... 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]

Protocol

Animal Research:

[3]

+ Expand
  • Animal Models: Naïve adult male AGMs
  • Formulation: 1N hydrochloride and carboxymethyl cellulose
  • 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
0.5% CMC Na (1N HCl, PH 2.5-3.0)
8mg/mL

* 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
Formula

C20H22N2O5

CAS No. 1044870-39-4
Storage powder
in solvent
Synonyms RVX-000222

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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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID