Catalog No.S4021 Synonyms: Ro 40-7592
Molecular Weight(MW): 273.24
Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
Purity & Quality Control
Choose Selective Transferase Inhibitors
|Description||Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.|
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.  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. 
|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.  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.  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). |
-  Zürcher G, et al. Adv Neurol, 1990, 53:497-50
-  Vieira-Coelho MA, et al. Br J Pharmacol, 1996, 117(3), 516-520.
-  Brannan T, et al. Neurology, 1992, 42(3 Pt 1), 683-685.
|In vitro||DMSO||55 mg/mL (201.28 mM)|
|Ethanol||55 mg/mL (201.28 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02740582||Recruiting||Alcohol Abuse|Impulsive Behavior||University of California, San Francisco||October 2016||--|
|NCT02949934||Recruiting||Alcohol Use Disorder||Medical University of South Carolina|National Institute on Alcohol Abuse and Alcoholism (NIAAA)||May 2016||Phase 2|
|NCT02630043||Recruiting||Neuroblastoma||Spectrum Health Hospitals||December 2015||Phase 1|
|NCT02652598||Enrolling by invitation||Brain Injuries, Traumatic|Neurocognitive Disorders|Brain Injuries||Sheppard Pratt Health System|Lieber Institute for Brain Development (LIBD)||November 2015||Phase 2|
|NCT02448654||Recruiting||Nicotine Dependence||Yale University|VA Office of Research and Development||October 2015||--|
|NCT02260570||Recruiting||Mild Traumatic Brain Injury||VA Office of Research and Development|University of California, Berkeley|University of California, San Francisco||August 2015||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.