Tolcapone是一种口服有效、选择性且强效的儿茶酚-O-甲基转移酶抑制剂，其IC₅₀值为773 nM，Ki值为30 nM。该化合物能够抑制α-突触核蛋白和β-淀粉样蛋白42的寡聚化及纤维化过程，同时可通过诱导氧化应激、促进活性氧生成和触发细胞凋亡等机制发挥抗肿瘤作用。托卡朋在帕金森病和神经母细胞瘤等神经系统疾病及肿瘤研究中具有重要应用价值。
| 英文别名 (English Synonym) | Tolcapone |
| 中文名称 (Chinese Name) | 托卡朋 |
| 靶点 (Target) | Transferase |
| 通路 (Pathway) | Protease/Metabolic Enzyme |
| CAS号 (CAS NO.) | 134308-13-7 |
| 分子式 (Formula) | C14H11NO5 |
| 分子量 (Molecular Weight) | 273.24 |
| 纯度 (Purity) | ≥98% |
| 溶解性 (Solubility) | 溶于DMSO |
-25~-15℃保存，有效期3年
[1] Di Giovanni S, Eleuteri S, Paleologou KE, Yin G, Zweckstetter M, Carrupt PA, Lashuel HA. 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 May 14;285(20):14941-14954. doi: 10.1074/jbc.M109.080390. Epub 2010 Feb 11. PMID: 20150427; PMCID: PMC2865316.
[2] Maser T, Rich M, Hayes D, Zhao P, Nagulapally AB, Bond J, Saulnier Sholler G. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in Neuroblastoma. Cancer Med. 2017 Jun;6(6):1341-1352. doi: 10.1002/cam4.1065. Epub 2017 Apr 21. PMID: 28429453; PMCID: PMC5463066.
