Tolcapone  (Synonyms: Ro 40-7592)

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].

COMT^[1]
α-syn and Aβ42 oligomerization, fibrillogenesis^[2]

Tolcapone is cytotoxic to neuroblastoma (NB) cells with IC₅₀ values ranging from 32.27 μM for SMS-KCNR cells to 219.8 μM for MGT9-102-08 primary cells^[3].
Tolcapone (25, 50,75, 100 μM) treatment activates downstream apoptotic events in NB cells. Tolcapone induces caspase-mediated apoptosis in neuroblastoma^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tolcapone (125 mg/kg; orally) inhibits tumor growth and prolongs survival in vivo. There are no adverse events or differences in weight or behavior noted in the mice^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

273.24

Solid

C₁₄H₁₁NO₅

134308-13-7

O=C(C1=CC(O)=C(O)C([N+]([O-])=O)=C1)C2=CC=C(C)C=C2

Room temperature in continental US; may vary elsewhere.

• [1]. 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.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]