Entacapone sodium salt

- Overview
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    Background
    
    Entacapone, a nitrocatechol compound, is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT), a Mg2+-dependent enzyme involved in the metabolism of catecholamines and catechol compounds, with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 20.1 nM and 10.7 nM respectively [1 & 2]. The nitro group at the position ortho to the hydroxyl group in the chemical structure of entacapone has been identified as a critical component for its potency and ability to inhibit COMT [2].Entacapone is an FDA-approved COMT inhibitor for use as an adjunct to levodopa therapy in patients’ with Parkinson’s disease, where it increases both the peripheral and central availability of levodopa [2].
    
    [1] Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Järvinen T, Männistö PT. Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506.
    [2] Najib J. Entacapone: a catechol-O-methyltransferase inhibitor for the adjunctive treatment of Parkinson's disease. Clin Ther. 2001 Jun;23(6):802-32; discussion 771.
- Properties
  - Alternative Name
    
    sodium (E)-5-(2-cyano-3-(diethylamino)-3-oxoprop-1-en-1-yl)-2-hydroxy-3-nitrophenolate
    
    CAS Number
    
    1047659-02-8
    
    Molecular Formula
    
    C14H14N3NaO5
    
    Molecular Weight
    
    327.27
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Entacapone sodium salt

Background

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