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XML generation date: 2024-04-24 09:10:45.663
Product last modified at: 2024-05-30T07:15:59.782Z
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PDP - Template Name: Chemical Modulators
PDP - Template ID: *******c501c72
  1. Products /
  2. Activators & Inhibitors /
  3. RVX-208

RVX-208 #76889

    Product Information

    Product Usage Information

    RVX-208 is supplied as a lyophilized powder. For a 20 mM stock, reconstitute 10 mg of powder in 1.35 ml of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

    Storage

    Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 370.4 g/mol
    Purity >98%
    Molecular Formula C20H22N2O5
    CAS 1044870-39-4
    Solubility Soluble in DMSO at 75 mg/ml or ethanol at 4 mg/ml.

    Background

    RVX-208 is a potent and selective inhibitor of bromodomain and extra terminal (BET) proteins, with a much stronger affinity for BD2 (IC50 = 0.510 μM) over BD1 (IC50 = 87 μM) (1,2). BET proteins interact with acetylated lysine-containing sequences to transcriptionally regulate several cellular processes. BRD4, a BET protein that mediates induction of Apolipoprotein A-I (ApoA-I) mRNA, can be disrupted at the binding site by RVX-208. This leads to altered transcription, resulting in increased ApoA-I production and high-density lipoprotein cholesterol (HDL-C) levels, both of which are promising in the treatment of atherosclerosis and vascular inflammation (2-4). Recently, BRD4 inhibition has shown anti-viral activity and increased host resistance to several DNA and RNA viruses in vitro and in vivo, making BRD4 disruptors important compounds to study in relation to viral diseases (5).

    限制使用

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    For Research Use Only. Not For Use In Diagnostic Procedures.
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