Entacapone

SKU: orb1226575

Description

Entacapone is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson's disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor. (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.(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 130929-57-6
• MW: 305.29
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₅N₃O₅
• SMILES: O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1
• Target: Transferase
• Solubility: Ethanol: 2 mg/mL (6.55 mM); DMSO: 61 mg/mL (199.81 mM)

Bioactivity

• 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. Animal model: High-fat diet-induced obese (DIO) mouse model. Dosage: 600 mg/kg. Administration: Oral administration; 600 mg/kg per day; 3-9 weeks. Result: Regulated the metabolic disorders in DIO mouse.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OR-611

Quick Database Links

Gene Symbol

Transferase