1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Apoptosis
  2. COMT
    Amyloid-β
    Apoptosis
  3. Tolcapone

Tolcapone (Synonyms: Ro 40-7592)

Cat. No.: HY-17406 Purity: 99.74%
Handling Instructions

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. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma.

For research use only. We do not sell to patients.

Tolcapone Chemical Structure

Tolcapone Chemical Structure

CAS No. : 134308-13-7

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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 114 In-stock
Estimated Time of Arrival: December 31
100 mg USD 150 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tolcapone

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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]

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].

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

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (365.98 mM; Need ultrasonic)

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
10 mM 0.3660 mL 1.8299 mL 3.6598 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are provided by MCE.
References

Purity: 99.74%

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Tolcapone
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