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> Tolcapone [134308-13-7]

Tolcapone [134308-13-7]

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Referência HY-17406-50mg

Tamanho : 50mg

Marca : MedChemExpress

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Description

Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma[1][2][3][4].

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]
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
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]
Sf21 IC50
119.6 μM
Compound: Tolcapone
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
Sf21 IC50
47.2 μM
Compound: Tolcapone
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
[PMID: 21965623]
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 (10-100 μM, 72 h) inhibits α-synuclein (α-syn) fibrillization[2].
Tolcapone (10-50 μM, 3 h) inhibits α-syn seed-induced polymerization[2].
Tolcapone (5-20 μM, 48 h) inhibits Aβ42 fibrillization[2].
Tolcapone (20 μM, 3 h) inhibits Aβ42 seed-induced polymerization[2].
Tolcapone (5-40 μM, 24 h) protects PC12 cells against α-syn and Aβ42-induced toxicity[2].
Tolcapone (1.5625-400 μM, 48 h) inhibits the viability of SMS-KCNR, SH-SY5Y, BE (2)-C, CHLA-90, MGT-015-08 and MGT9-102-08 neuroblastoma cells, with IC50 values of 32.27-219.8 μM[4].
Tolcapone (1.5625-400 μM, 48 h) inhibits neuroblastoma cell proliferation with GI50 values of 34-130 μM[4].
Tolcapone (25-400 μM, 48 h) induces apoptosis in neuroblastoma cells[4].
Tolcapone (50-100 μM, 1-3 h) increases ROS levels in BE (2)-C and SMS-KCNR cells[4].
Tolcapone (50-200 μM, 48 h) decreases the ATP per cell ratio in neuroblastoma cells[4].

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

Tolcapone Related Antibodies

Apoptosis Analysis[1]

Cell Line: SMS-KCNR, SH-SY5Y, BE (2)-C, CHLA-90, MGT-015-08 and MGT9-102-08 neuroblastoma cells
Concentration: 25, 50, 75, 100, 200 and 400 μM
Incubation Time: 48 h
Result: Increased dead cells by SYTOX Green staining and increased apoptotic cells by caspase-3/7 reagent.
Increased the expression of cleaved caspase-3 and cleaved PARP.
Decreased the expression of full-length caspase-3 and full-length PARP.
In Vivo

Tolcapone (125 mg/kg, i.g., once daily) inhibits tumor growth and prolongs survival in SMS-KCNR xenograft mice models[4].

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

Animal Model: SMS-KCNR xenograft mice models[4]
Dosage: 125 mg/kg
Administration: Orally gavage, once daily
Result: Reduced tumor volume.
Prolonged survival of mice.
Showed no abnormal weight or behavior.
Essai clinique
Masse moléculaire

273.24

Formule

C14H11NO5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
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.
Pureté et documentation
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