Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Tolcapone (Ro 40-7592; SOM-0226; Ro-407592; Tasmar), an approved anti-Parkinson's disease (PD) agent, is a reversible and orally bioavailable inhibitor of catechol-O-methyl transferase (COMT) with potential anti-PD effects. It inhibits COMT with Ki of 30 NM. COMTcatalyses a relatively minor pathway of dopamine metabolism, therefore the action of dopamine can be enhanced by tolcapone. Tolcapone is used in combination with levodopa for the treatment of Parkinson's disease (PD).
ln Vitro |
Neuroblastoma (NB) cells are cytotoxic to tolcapone; its IC50 values range from 32.27 μM for SMS-KCNR cells to 219.8 μM for primary MGT9-102-08 cells[3]. In NB cells, tolcapone (25, 50, 75, and 100 μM) treatment triggers subsequent apoptotic processes. In neuroblastoma, tolcapone triggers caspase-mediated apoptosis[3].
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ln Vivo |
Oral tolcapone (125 mg/kg) suppresses the growth of tumors and increases in vivo survival. The mice's weight or behavior have not changed, nor have any unfavorable events been reported[3].
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Cell Assay |
Cell Viability Assay[3]
Cell Types: BE(2)-C, SMS-KCNR, CHLA-90, SH-SY5Y, MGT-015 -08 and MGT9-102-08 Tested Concentrations: 1.5625~400 μM Incubation Duration: 48 hrs (hours) Experimental Results: IC50s of 32.27, 72.31, 80.29, 109.4, 174.6, 219.8 μM for SMS-KCNR, SH-SY5Y, BE(2)-C, CHLA-90, MGT-015-08 and MGT9-102-08, respectively. Cell Viability Assay[3] Cell Types: NB Cell Types: BE(2)-C, SMS-KCNR, CHLA-90, SH-SY5Y, MGT-015-08 and MGT9-102-08 Tested Concentrations: 25, 50, 75, 100 μM Incubation Duration: Experimental Results: A dose-dependent increase in cleaved caspase-3 and cleaved PARP protein in all six NB cell lines and a subsequent decrease in whole caspase-3 and whole PARP protein. |
Animal Protocol |
Animal/Disease Models: 4weeks old female nude mice (nu /nu) bearing SMS‐KCNR xenograft models [3]
Doses: 125 mg/kg Route of Administration: Treated orally every 24 h for 35 days Experimental Results: diminished tumor volume compared to control. Resulted in a smaller average tumor of 490±310 mm3 compared to control tumors of 1100±450 mm3. |
References |
[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.
[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. [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. |
Molecular Formula |
C14H11NO5
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Molecular Weight |
273.24
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CAS # |
134308-13-7
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Related CAS # |
Tolcapone-d7;Tolcapone-d4;1246816-93-2
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SMILES |
O=C(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])C1C([H])=C(C(=C(C=1[H])[N+](=O)[O-])O[H])O[H]
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InChi Key |
MIQPIUSUKVNLNT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H11NO5/c1-8-2-4-9(5-3-8)13(17)10-6-11(15(19)20)14(18)12(16)7-10/h2-7,16,18H,1H3
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Chemical Name |
(3,4-dihydroxy-5-nitrophenyl)-(4-methylphenyl)methanone
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6598 mL | 18.2989 mL | 36.5979 mL | |
5 mM | 0.7320 mL | 3.6598 mL | 7.3196 mL | |
10 mM | 0.3660 mL | 1.8299 mL | 3.6598 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.