Entacapone

Cat. No. 4720

Entacapone C14H15N3O5 [130929-57-6]

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Chemical Name: (2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide

Biological Activity

Potent catechol O-methyltransferase (COMT) inhibitor (IC50 values are 14.3, 20.1 and 73.3 nM for rat liver soluble COMT, total COMT and membrane-bound COMT respectively). Increases bioavailability of levodopa when given as an adjunct therapy for Parkinson's disease. Inhibits α-synuclein aggregation in an in vitro assay; blocks α-synuclein-induced cell death in PC-12 cells.

Technical Data

M.Wt:
305.29
Formula:
C14H15N3O5
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>99 %
Storage:
Store at RT
CAS No:
130929-57-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Di Giovanni et al (2010) 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. 285 14941. PMID: 20150427.

Forsberg et al (2003) Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J.Pharmacol.Exp.Ther. 304 498. PMID: 12538800.

Merello et al (1994) Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with levodopa in patients with Parkinson's disease. J.Neurol.Neurosurg.Psychiatry 57 186. PMID: 8126502.

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Keywords: Entacapone, supplier, potent, catechol, O, methyltransferase, COMT, inhibitors, inhibits, Parkinsons, disease, alpha, synuclein, a-syn, aggregation, 3-O-methyldopa, parkinson's, Tocris Bioscience, Catechol O-Methyltransferase Inhibitor products

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