Entacapone

Name: Entacapone
Brand: Tocris Bioscience
SKU: 4720

Tocris Bioscience, part of Bio-Techne | Catalog # 4720

Citations (5)

COA / SDS

Potent COMT inhibitor; blocks α-synuclein aggregation

Key Product Details

Description:	Potent COMT inhibitor; blocks α-synuclein aggregation
Chemical Name:	(2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide
Purity:	≥99% (HPLC)
Molecular Weight:	305.29

View Full Technical Details for Entacapone

Technical Data
Citations

Biological Activity for Entacapone

Entacapone is a 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 for Entacapone

M. Wt	305.29
Formula	C₁₄H₁₅N₃O₅
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	130929-57-6
PubChem ID	5281081
InChi Key	JRURYQJSLYLRLN-BJMVGYQFSA-N
Smiles	OC1=CC(/C=C(C#N)/C(N(CC)CC)=O)=CC([N+]([O-])=O)=C1O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Entacapone

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	30.53	100
	ethanol	3.05	10

Preparing Stock Solutions for Entacapone

The following data is based on the product molecular weight 305.29.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.28 mL	16.38 mL	32.76 mL
5 mM	0.66 mL	3.28 mL	6.55 mL
10 mM	0.33 mL	1.64 mL	3.28 mL
50 mM	0.07 mL	0.33 mL	0.66 mL

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References for Entacapone

References are publications that support the biological activity of the product.

Forsberg Pharmacokinetics and pharmacodynamics of entac. and tolc. after acute and repeated administration: a comparative study in the rat. J.Pharmacol.Exp.Ther. 2003 PMID: 12538800
Merello Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with lev. in patients with Parkinson's disease. J.Neurol.Neurosurg.Psychiatry 1994 PMID: 8126502
Di Giovanni 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 PMID: 20150427