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Tolcapone

Catalog No. T6708 CAS 134308-13-7

Synonyms: Tasmar, Ro 40-7592

Tolcapone (Ro 40-7592) is a catechol-O-methyltransferase inhibitor used in the therapy of Parkinson disease as adjunctive therapy in combination with levodopa and carbidopa.

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Tolcapone, CAS 134308-13-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 45.00
25 mg	In stock	$ 79.00
50 mg	In stock	$ 98.00
100 mg	In stock	$ 133.00
200 mg	In stock	$ 189.00
500 mg	In stock	$ 316.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.89%

Purity: 99.49%

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Description	Tolcapone (Ro 40-7592) is a catechol-O-methyltransferase inhibitor used in the therapy of Parkinson disease as adjunctive therapy in combination with levodopa and carbidopa.
Targets&IC50	COMT:30 nM(Ki)
In vitro	Tolcapone functions as a selective peripheral and central COMT inhibitor, exerting no effect on adrenergic, serotonergic, or cholinergic receptors or other enzymes involved in synthesis or catabolism of catecholamines. [1] Tolcapone produces a concentration-dependent decrease in COMT activity in liver homogenates of developing (3 days-old) and adult (60 days-old) rats with Vmax, Km and IC50 of 5.3 nM/mg/h, 3.3 μM, 41 nM, and 2.9 nM/mg/h, 13.1 μM, 720 nM, respectively. Tolcapone produces a concentration-dependent decrease in COMT activity in kidney of developing (3 days-old) and adult (60 days-old) rats with Vmax, Km and IC50 of 2.6 nM/mg/h, 2.7 μM, 8 nM, and 3.5 nM/mg/h, 24 μM, 177 nM, respectively. [2]
In vivo	Tolcapone orally administrated is able to crosses the blood-brain barrier. Acute administration of Tolcapone increases basal levels of L-DOPA and dihydroxyphenylacetic acid (DOPAC) and decreases basal homovanillic acid (HVA) levels, but does not affect basal dopamine levels. [3] Tolcapone (30 mg/kg p.o.) combined with benserazide (15 mg/kg p.o.) and a low dose of L-dopa (10 mg/kg p.o.) almost completely blockes (for about 6 h) the formation of 3-O-methyldopa (3-OMD) in brain and plasma, producing a long-lasting increase of L-DOPA in plasma and a parallel marked increase of L-DOPA and dopamine in the brain. [4] Tolcapone displays behavioural and neurochemical benefits on animals. Tolcapone (30 mg/kg p.o.) increases the effect of L-DOPA (plus benserazide) on locomotor activity, reserpine-induced hypothermia, and catalepsy induced by pimozide, haloperidol and fluphenazine. Tolcapone also increases locomotor hyperactivity induced by amphetamine or nomifensine, as well as stereotypy induced by amphetamine (but not apomorphine). [5]
Kinase Assay	Enzyme assay and binding assay: Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine.

Synonyms	Tasmar, Ro 40-7592
Molecular Weight	273.24
Formula	C14H11NO5
CAS No.	134308-13-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 27.3 mg/mL (100 mM)

DMSO: 27.3 mg/mL (100 mM)

References and Literature

1. Zürcher G, et al. Adv Neurol, 1990, 53:497-50 2. Vieira-Coelho MA, et al. Br J Pharmacol, 1996, 117(3), 516-520. 3. Brannan T, et al. Neurology, 1992, 42(3 Pt 1), 683-685. 4. Zürcher G, et al. J Neural Transm Suppl, 1990, 32, 375-38 5. Maj J, et al. J Neural Transm Park Dis Dement Sect, 1990, 2(2), 101-112. 6. Qiu M, Li Z, Chen Y, et al. Tolcapone Potently Inhibits Seminal Amyloid Fibrils Formation and Blocks Entry of Ebola Pseudoviruses. Frontiers in Microbiology. 2020, 11: 504.

Citations

1. Qiu M, Li Z, Chen Y, et al. Tolcapone Potently Inhibits Seminal Amyloid Fibrils Formation and Blocks Entry of Ebola Pseudoviruses. Frontiers in Microbiology. 2020, 11: 504

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Neurodegenerative Disease Compound Library EMA Approved Drug Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Parkinson's Disease Compound Library Drug-induced Liver Injury (DILI) Compound Library

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Keywords

Tolcapone 134308-13-7 Apoptosis Metabolism Neuroscience Transferase Beta Amyloid central COMT Peripheral methyltransferase Tasmar Ro 40-7592 inhibit stress Abeta Inhibitor oxidative Neuroblastoma Amyloid-β β-amyloid peptide inhibitor

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