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  3. Apabetalone

Apabetalone (Synonyms: RVX-208; RVX000222)

Cat. No.: HY-16652 Purity: 99.33%
Handling Instructions

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.

For research use only. We do not sell to patients.

Apabetalone Chemical Structure

Apabetalone Chemical Structure

CAS No. : 1044870-39-4

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10 mM * 1 mL in DMSO USD 90 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Apabetalone purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.

    RVX208 increases CTGF and CYR61 expression and TAZ protein level in HCT116 cells.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.

    IC50 & Target

    IC50: 510±41 nM (BD2), 87±10 μM (BD1)[1]

    In Vitro

    Apabetalone (RVX-208) competes with binding of an acetylated histone peptide to tandem BD1 BD2 protein constructs of the four BET proteins, with IC50s between 0.5 and 1.8 µM. Apabetalone increases the production of ApoA-I in hepatocytes in vitro, which results in increased high density lipoprotein cholesterol (HDL-C). Apabetalone selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. Apabetalone increases Apolipoprotein A-I (ApoA-I) production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Apabetalone increases ApoA-I expression in liver cells[2].

    In Vivo

    In the atherosclerosis prophylactic treatment study design, mice are fed a Western diet concurrent with the treatment with 150 mg/kg/dose b.i.d. for 12 weeks. Mice are sacrificed at 12 weeks after treatment. There is a progressive increase in body weight in both the vehicle treated as well as the Apabetalone (RVX-208) treated groups. However, there is only an increase of 4 g (from 24 g to 28 g) body weight after 12 weeks on Western diet in the Apabetalone treated group whereas this increase is found to be 9 g (25 g-34 g) in the vehicle treated group. The significant decrease in body weight gain in Apabetalone treated mice is not due to decreased feed consumption, suggesting a positive attribute of the molecule. Plasma lipid measurements are done at 6 weeks and 12 weeks of treatment with either the vehicle or Apabetalone. Compared to the vehicle control animals, Apabetalone treated mice show significant increase (~200%) in the levels of HDL-C at 6 weeks of treatment, which is sustained until end of the study (12 weeks)[3].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (89.09 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6998 mL 13.4989 mL 26.9978 mL
    5 mM 0.5400 mL 2.6998 mL 5.3996 mL
    10 mM 0.2700 mL 1.3499 mL 2.6998 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 µM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 µg/mL for 3 hours[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    Seven to eight week old male ApoE-/- mice are used. Based on the body weight and lipid values, mice are divided into 2 groups (n=12): group 1, vehicle; and group 2, test agent, Apabetalone. Mice are then switched to Western diet (0.15% cholesterol and 42% calories from fat) and concurrently treated orally by gavage with either vehicle or the test agent, Apabetalone (150 mg/kg/dose b.i.d) for 12 weeks. After 6 week of treatment, an interim blood draw is done to monitor serum lipid levels. After 12 weeks of treatment mice are sacrificed to measure blood lipid parameters, aortic lesion, and liver and aortic RNA. Eight mice are used for enface (aortic plaque) analysis, 4 mice for tissue collection for mRNA and all 12 mice used for aortic sinus lesion area measurement.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    370.40

    Formula

    C₂₀H₂₂N₂O₅

    CAS No.

    1044870-39-4

    SMILES

    COC1=CC(OC)=C(C(NC(C2=CC(C)=C(OCCO)C(C)=C2)=N3)=O)C3=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.33%

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    Product Name:
    Apabetalone
    Cat. No.:
    HY-16652
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    Apabetalone

    Cat. No.: HY-16652