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Submit ReviewEntacapone
说明： Potent COMT inhibitor; blocks α-synuclein aggregation
化学名： (2E)-2-Cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide
纯度： ≥99% (HPLC)
生物活性 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.
技术数据 for Entacapone
| 分子量 | 305.29 |
| 公式 | C14H15N3O5 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Entacapone
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 30.53 | 100 | |
| ethanol | 3.05 | 10 |
制备储备液 for Entacapone
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Entacapone
参考文献 for Entacapone
参考文献是支持产品生物活性的出版物。
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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关键词: 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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.