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Entacapone sodium salt CAS: 1047659-02-8

Category: Inhibitors
Product Name: Entacapone sodium salt
Cat No: I000267
CAS No: 1047659-02-8
Synonyms: sodium (E)-5-(2-cyano-3-(diethylamino)-3-oxoprop-1-en-1-yl)-2-hydroxy-3-nitrophenolate
Molecular Formula: C14H14N3NaO5
Molecular Weight: 327.27
SMILES: CCN(C(/C(C#N)=C([H])/C1=CC(N(=O)=O)=C(O)C([O-])=C1)=O)CC.[Na+]
Solubility: 10 mM in DMSO
Target: COMT
IC50: 151 nM
Storage: Store at -20°C
CAS 1047659-02-8,Entacapone sodium salt
  • Description

Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.
IC50 Value: 151 nM
Target: COMT
in vitro: Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
in vivo: Levodopa/carbidopa/entacapone has been shown to improve the pharmacokinetic profile of levodopa and provide superior symptomatic control compared with conventional levodopa/dopa decarboxylase inhibitor therapy. We report four case histories describing clinical experience of using levodopa/carbidopa/entacapone 200/50/200 mg, one of the latest doses of this formulation, in a range of patients with Parkinson's disease. These cases illustrate that levodopa/carbidopa/entacapone 200/50/200 mg provides improvements in symptomatic control.
Clinical trial: The combination product carbidopa/levodopa/entacapone (CLE) was approved in 2003 for the treatment of PD patients.

  • References


[1]. Di Giovanni, S., et al., Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. J Biol Chem, 2010. 285(20): p. 14941-54.
[2]. Jenner, P., Avoidance of dyskinesia: preclinical evidence for continuous dopaminergic stimulation. Neurology, 2004. 62(1 Suppl 1): p. S47-55.
[3]. Hamaue, N., et al., Entacapone, a catechol-O-methyltransferase inhibitor, improves the motor activity and dopamine content of basal ganglia in a rat model of Parkinson's disease induced by Japanese encephalitis virus. Brain Res, 2010. 1309: p. 110-5.


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