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Technical Data
| Formula |
C14H11NO5
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| Molecular Weight | 273.24 | CAS No. | 134308-13-7 | |
| Solubility (25°C)* | In vitro | DMSO | 55 mg/mL (201.28 mM) | |
| Ethanol | 55 mg/mL (201.28 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. | ||
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| Targets |
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| 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] |
Protocol (from reference)
References
Selleck's Tolcapone has been cited by 3 publications
| Entacapone alleviates acute kidney injury by inhibiting ferroptosis [ FASEB J, 2022, 36(7):e22399] | PubMed: 35691001 |
| Inhibitors of Venezuelan Equine Encephalitis Virus Identified Based on Host Interaction Partners of Viral Non-Structural Protein 3 [ Viruses, 2021, 13(8)1533] | PubMed: 34452398 |
| Differential Interactome Based Drug Repositioning Unraveled Abacavir, Exemestane, Nortriptyline Hydrochloride, and Tolcapone as Potential Therapeutics for Colorectal Cancers [ Front Bioinform, 2021, 1:710591] | PubMed: 36303724 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.