1. Metabolic Enzyme/Protease Neuronal Signaling
  2. COMT
  3. Entacapone sodium salt

Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.

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CAS No. : 1047659-02-8

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Top Publications Citing Use of Products

    Entacapone sodium salt purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3640-3656.  [Abstract]

    The rate of NADH to NAD+ conversion rate measuring the mitochondrial complex I activity using mitochondrial extracts from U87 cells treated with DMSO, 50 μmol/L Entacapone, or 100 μmol/L Tolcapone for 24 hours.

    Entacapone sodium salt purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3640-3656.  [Abstract]

    ROS flow cytometry assay comparing the ROS production of U87 cells treated with DMSO (control) or 50 μmol/L Entacapone for 24 hours.

    Entacapone sodium salt purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3640-3656.  [Abstract]

    Immunofluorescence showing the localization of the mitochondria (as detected by HSP60) and dsRNA (as detected by J2) in the cytoplasm of VC, COMT-KO, Act-D–treated VC, Act-D–treated COMT-KO U87 cells (top), and wild-type U87 cells treated with DMSO or 50 µmol/L Entacapone for 24 hours (bottom).

    Entacapone sodium salt purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3640-3656.  [Abstract]

    Quantification of the percentage of macrophages that phagocytosed CT2A cells treated with DMSO, 50 µmol/L Entacapone, or 50 µmol/L Tolcapone. CT2A cells were pretreated with COMT inhibitors for 24 hours prior to coculturing with macrophages.

    Entacapone sodium salt purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3640-3656.  [Abstract]

    The drug treatment and irradiation schedule in mice bearing subcutaneous CT2A tumors. Vehicle and 30 mg/kg Entacapone were administered intraperitoneally daily from day 3 to day 35. The tumor-bearing right flank was irradiated on day 10 post tumor cell inoculation. IP, intraperitoneal injection; q.d., every day; IR, irradiation.

    Entacapone sodium salt purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3640-3656.  [Abstract]

    Tumor growth of C57BL/6 mice (n = 6) subcutaneously implanted with 5 × 105 CT2A cells and received Entacapone and Radiotherapy treatments.
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    Description

    Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease[1]. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].

    IC50 & Target

    IC50: 10 nM (rat brain COMT); 20 nM (rat erythrocyte COMT); 160 nM (rat liver COMT)[1]

    In Vitro

    Entacapone sodium salt (50 μM, 48 hours) enhances the amount of m6A on mRNA in Hep-G2 cells. It does not show any inhibitory effect on the enzymatic activity of the RNA m6A demethylase AlkB homolog 5 (ALKBH5) or the ten-eleven translocation methylcytosine dioxygenase 1 (TET1), nor does it alter the DNA methylation or histone methylation patterns in Entacapone sodium salt -treated Hep-G2 cells[2].

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

    In Vivo

    Entacapone sodium salt (oral administration; 600 mg/kg per day; 3-9 weeks) results in a dose-response effect dose-response effect. After 3 weeks, mouse body weight are decreased by 10.1% compared to controls, and shows similar food intake  fat mass and fat mass ratio reduced after Entacapone sodium salt treatment. Entacapone sodium salt also increases the energy expenditure of mice: reductions in total cholesterol (17.6%), low-density lipoprotein cholesterol (31.0%), and triglycerides (10.2%) in mice[2].

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

    Clinical Trial
    Molecular Weight

    327.27

    Formula

    C14H14N3NaO5

    CAS No.
    SMILES

    O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C([O-])C(O)=C1.[Na+]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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