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    Apabetalone (RVX-08, RVX-000222)
    Apabetalone (RVX-08, RVX-000222)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0415
    CAS #: 1044870-39-4 Purity ≥98%

    Description: Apabetalone (also known as RVX-208, RVX000222) is a novel and potent inhibitor of BET (Bromodomain and Extra-Terminal) bromodomain (BD) with potential anti-inflammatory activity and the potential to be used in the treatment of cardiovascular diseases. It inhibits BET (BD2) with an IC50 of 0.510 μM in a cell-free assay, and shows about 170-fold higher selectivity for BD2 over BD1. RVX-208 is currently undergoing phase III clinical trials for reducing the relative risk (RR) of major adverse cardiac events (MACE) in patients with cardiovascular disease (CVD). It acts by binding to the acetyl-lysine binding pocket in a peptide-competitive way. In HepG2 cells, RVX-208 induced messenger ribonucleic acid and protein synthesis of apolipoprotein (apo)A-I. 

    References: Proc Natl Acad Sci U S A. 2013;110(49):19754-9; Curr Opin Investig Drugs. 2010;11(3):357-64.

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    Molecular Weight (MW)370.4
    FormulaC20H22N2O5
    CAS No.1044870-39-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 0.5% CMC Na (1N HCl, PH 2.5-3.0): 8 mg/mL
    Synonyms

    RVX-000222; RVX208; RVX 000222; RVX 208; RVX000222; RVX-208; Apabetalone.

    Chemical Name: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one

    InChi Key: NETXMUIMUZJUTB-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24)

    SMILES Code: O=C1NC(C2=CC(C)=C(OCCO)C(C)=C2)=NC3=C1C(OC)=CC(OC)=C3 


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: Experiments are run on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. IC50 values are calculated in Prism 5 after normalization against corresponding DMSO controls. Assays are performed according to the manufacturer’s protocol with minor modifications.


    Cell Assay: HepG2 cells treated with RVX-208 (5 μM) for 4 h only modestly affected BET-dependent gene transcription. Moreover, RVX-208 increased apolipoprotein (apo)A-I and high-density lipoprotein cholesterol (HDL-C) levels in HepG2 cells.

    In VivoRVX-208 significantly increases serum apoA-I and HDL-C in AGMs, and enhances cholesterol efflux via different pathways.
    Animal modelNaïve adult male AGMs
    Formulation & DosageDissolved in 1N HCl and carboxymethyl cellulose; 60mg/kg;  i.v. injection or p.o.
    References

    Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9; Curr Opin Investig Drugs. 2010 Mar;11(3):357-64; J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    RVX-208

    RVX-208


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