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

Entacapone 

Cat. No.: HY-14280 Purity: 99.97%
Handling Instructions

Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone 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 can be used for the research of Parkinson's disease. Entacapone serves as a inhibits FTO demethylation activity with an IC50 of 3.5 μM and can be used for the research of metabolic disorders.

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

Entacapone Chemical Structure

Entacapone Chemical Structure

CAS No. : 130929-57-6

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Based on 1 publication(s) in Google Scholar

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Description

Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone 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 can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibits FTO demethylation activity with an IC50 of 3.5 μM and 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 (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-treated Hep-G2 cells[2].

In Vivo

Entacapone (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 treatment. Entacapone 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].

Animal Model: High-fat diet-induced obese (DIO) mouse model[2]
Dosage: 600 mg/kg
Administration: Oral administration; 600 mg/kg per day; 3-9 weeks
Result: Regulated the metabolic disorders in DIO mouse.
Clinical Trial
Molecular Weight

305.29

Formula

C₁₄H₁₅N₃O₅

CAS No.

130929-57-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

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 : 33.33 mg/mL (109.17 mM; Need ultrasonic)

H2O : 2 mg/mL (6.55 mM; ultrasonic and adjust pH to 10 with NaOH)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2756 mL 16.3779 mL 32.7557 mL
5 mM 0.6551 mL 3.2756 mL 6.5511 mL
10 mM 0.3276 mL 1.6378 mL 3.2756 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (8.19 mM); Clear solution; Need warming

*All of the co-solvents are provided by MCE.
References

Purity: 99.97%

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Keywords:

EntacaponeCOMTCatechol-O-methyltransferasemetabolic disorderParkinson's disease?FTO?knockdownInhibitorinhibitorinhibit

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