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Submit ReviewEntacapone
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)
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 Data 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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Product Datasheets for Entacapone
References for Entacapone
References are publications that support the biological activity of the product.
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 entac. and tolc. 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 lev. in patients with Parkinson's disease. J.Neurol.Neurosurg.Psychiatry 57 186 PMID: 8126502
If you know of a relevant reference for Entacapone, please let us know.
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Keywords: Entacapone, Entacapone supplier, potent, catechol, O, methyltransferase, COMT, inhibitors, inhibits, Parkinsons, disease, alpha, synuclein, a-syn, aggregation, 3-O-methyldopa, parkinson's, Catechol, O-Methyltransferase, 4720, Tocris Bioscience
Citations for Entacapone
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.