A selective BET bromodomain antagonist
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RVX-208

Item No. 16424

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-4(3H)-quinazolinone
CAS Number
1044870-39-4
Synonyms
  • Apabetalone
  • RVX-000222
Molecular Formula
C20H22N2O5
Formula Weight
370.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/mlEthanol: 1 mg/ml
λmax
261, 309 nm
SMILES
O=C1C2=C(OC)C=C(OC)C=C2NC(C3=CC(C)=C(OCCO)C(C)=C3)=N1
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)
InChi Key
NETXMUIMUZJUTB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $120

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    10 mg

    $213

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    25 mg

    $445

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    Product Description

    RVX-208 is a selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 µM) over BD1 (IC50 = 1.8-3.1 µM).1,2 RVX-208 causes the selective release of BET proteins from chromatin in cells.1,2 It interferes with the BET protein BRD4, resulting in an increased expression of apolipoprotein (Apo) A1 in cells, mice, monkeys, and humans.3,4 RVX-208 also reduces atherosclerosis in hyperlipidemic ApoE-deficient mice.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McLure, K.G., Gesner, E.M., Tsujikawa, L., et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One 8(12), 1-12 (2013).

    2. Picaud, S., Wells, A., Felletar, I., et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc. Natl. Acad. Sci. USA 110(49), 19754-19759 (2013).

    3. Bailey, D., Jahagirdar, R., Gordon, A., et al. RVX-208: A small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J. Am. Coll. Cardiol. 55(23), 2580-2589 (2010).

    4. Jahagirdar, R., Zhang, H., Azhar, S., et al. A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice. Atherosclerosis 236(1), 91-100 (2014).