Tolcapone-d4Tolcapone-d4
MedChemExpress (MCE)
HY-17406S1
1246816-93-2
Ro 40-7592-d4
99.13%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
Tolcapone-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].
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].
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[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019
53(2):211-216. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]