Biological Activity
COMT inhibitor. Inhibits both brain and peripheral COMT. Also binds transthyretin (TTR) with high affinity (Kd1 and Kd2 values are 21 and 58 nM, respectively). Inhibits TTR aggregation in human plasma and prevents TTR-induced cytotoxicity in vitro. Stabilizes TTR in mice and humans in vivo. Orally bioavailable.
Technical Data
| M. Wt | 273.24 |
| Formula | C14H11NO5 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 134308-13-7 |
| PubChem ID | 4659569 |
| InChI Key | MIQPIUSUKVNLNT-UHFFFAOYSA-N |
| Smiles | OC1=C(O)C([N+]([O-])=O)=CC(C(C2=CC=C(C)C=C2)=O)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.32 | 100 | |
| ethanol | 27.32 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 273.24. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.66 mL | 18.3 mL | 36.6 mL |
| 5 mM | 0.73 mL | 3.66 mL | 7.32 mL |
| 10 mM | 0.37 mL | 1.83 mL | 3.66 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.73 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sant'Anna et al (2016) Repositioning tolcapone as a potent inhibitor of transthyretin amyloidogenesis and associated cellular toxicity. Nat.Commun. 7 10787 PMID: 26902880
Männistö et al (1992) Different in vivo properties of three new inhibitors of catechol O-methyltransferase in the rat. Br.J.Pharmacol. 105 569 PMID: 1628144
Keywords: Tolcapone, supplier, catechol, O-methyl, transferase, inhibitors, inhibits, COMT, orally, bioavailable, high, affinity, TTR, binding, transthyretin, aggregation, Ro40-7592, Tasmar, Ro, 40-7592, Catechol, O-Methyltransferase, Catechol, O-Methyltransferase, Tocris Bioscience
