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> Tolcapone [134308-13-7]

Tolcapone [134308-13-7]

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Cat# HY-17406-100mg

Size : 100mg

Brand : MedChemExpress

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Description

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].

IC50 & Target

COMT[1]
α-syn and Aβ42 oligomerization, fibrillogenesis[2]
Cellular Effect
Cell Line Type Value Description References
BHK-21 CC50
29.2 μM
Compound: 22
Cytotoxicity against golden hamster BHK-21 cells incubated for 24 hrs by CCK-8 assay
Cytotoxicity against golden hamster BHK-21 cells incubated for 24 hrs by CCK-8 assay
[PMID: 34458734]
HEK293 IC50
< 1 nM
Compound: 1
Inhibition of human MB-COMT expressed in HEK293 cells using dopamine as substrate and SAM as cofactor preincubated for 30 mins followed by substrate addition and measured after 40 mins by HTRF assay
Inhibition of human MB-COMT expressed in HEK293 cells using dopamine as substrate and SAM as cofactor preincubated for 30 mins followed by substrate addition and measured after 40 mins by HTRF assay
[PMID: 32038769]
HeLa CC50
> 25 μM
Compound: Tolcapone
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Blue assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Blue assay
[PMID: 33851839]
HeLa IC50
50 μM
Compound: Tolcapone
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
Inhibition of human KLF10 expressed in human HeLa cells assessed as reduction in transcriptional activity after 24 hrs by CACCC-responsive promoter driven TK-luciferase reporter gene assay
[PMID: 25581017]
HT-29 EC50
7.44 μM
Compound: Tolcapone
Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
10.1039/C2MD20210G
U2OS EC50
49.2 μM
Compound: Tolcapone
Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
10.1039/C2MD20210G
In Vitro

Tolcapone is cytotoxic to neuroblastoma (NB) cells with IC50 values ranging from 32.27 μM for SMS-KCNR cells to 219.8 μM for MGT9-102-08 primary cells[3].
Tolcapone (25, 50,75, 100 μM) treatment activates downstream apoptotic events in NB cells. Tolcapone induces caspase-mediated apoptosis in neuroblastoma[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tolcapone Related Antibodies

Cell Viability Assay[3]

Cell Line: BE(2)-C, SMS-KCNR, CHLA-90, SH-SY5Y, MGT-015-08 and MGT9-102-08
Concentration: 1.5625~400 μM
Incubation Time: 48 hours
Result: 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 Line: NB cell lines: BE(2)-C, SMS-KCNR, CHLA-90, SH-SY5Y, MGT-015-08 and MGT9-102-08
Concentration: 25, 50, 75, 100 μM
Incubation Time:
Result: 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.
In Vivo

Tolcapone (125 mg/kg; orally) inhibits tumor growth and prolongs survival in vivo. There are no adverse events or differences in weight or behavior noted in the mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-week-old female nude mice (nu/nu) bearing SMS‐KCNR xenograft models [3]
Dosage: 125 mg/kg
Administration: Treated orally every 24 h for 35 days
Result: Decreased tumor volume compared to control.
Resulted in a smaller average tumor of 490±310 mm3 compared to control tumors of 1100±450 mm3.
Clinical Trial
Molecular Weight

273.24

Formula

C14H11NO5
CAS No.
Appearance

Solid

Color

Colorless to light yellow

SMILES

O=C(C1=CC(O)=C(O)C([N+]([O-])=O)=C1)C2=CC=C(C)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (365.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

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