Tolcapone-d4(Synonyms: Ro 40-7592-d4)

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Tolcapone-d4 (Synonyms: Ro 40-7592-d4)

Tolcapone-d4 (Ro 40-7592-d4) 是 Tolcapone 的氘代物。Tolcapone (Ro 40-7592) 是一种选择性，有效的，具有口服活性的外周和中枢 COMT 抑制剂，在肝脏中对 COMT 的 IC50 为 773 nM。Tolcapone 还是一种 α-syn 和 Aβ42 寡聚和原纤维形成的有效抑制剂。Tolcapone 诱导氧化应激导致神经母细胞瘤细胞凋亡(apoptosis) 和抑制肿瘤生长。

Tolcapone-d4(Synonyms: Ro 40-7592-d4)

Tolcapone-d4 Chemical Structure

CAS No. : 1246816-93-2

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生物活性

Tolcapone-d4 (Ro 40-7592-d4) is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

277.27

Formula

C14H7D4NO5
CAS 号

1246816-93-2
中文名称

托卡朋 d4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Catechol-O-methyltransferase: variation in enzyme activity and inhibition by entacapone and tolcapone. C De Santi, et al. Eur J Clin Pharmacol. 1998 May;54(3):215-9.

    [3]. Saviana Di Giovanni, et al. 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.

    [4]. Tyler Maser,et al. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in Neuroblastoma.Cancer Med. 2017 Jun;6(6):1341-1352.

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