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    Apabetalone (RVX-208, RVX000222)
    Apabetalone (RVX-208, RVX000222)

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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, potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. RVX-208 binds 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. It is currently undergoing phase III clinical trials for the treatment of cardiovascular diseases.

    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
    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

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

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


    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.

    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.




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