1、TolcaponeCat. No.: HY-17406CAS No.: 134308-13-7Molecular Formula: CHNOMolecular Weight: 273.24Target: COMTPathway: Metabolic Enzyme/Protease; Neuronal SignalingStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent & SolubilityIn Vitro 10 mM in DMSOConcentrationSolvent Mas
2、s 1 mg 5 mg 10 mg1 mM 3.6598 mL 18.2989 mL 36.5979 mL5 mM 0.7320 mL 3.6598 mL 7.3196 mLPreparing Stock Solutions10 mM 0.3660 mL 1.8299 mL 3.6598 mLPlease refer to the solubility information to select the appropriate solvent.BIOLOGICAL ACTIVITYDescription Tolcapone(Ro 40-7592) is an orally active sel
3、ective, potent catechol-O-methyltransferase (COMT) inhibitor. IC50 value:Target: COMTTolcapone inhibits both central and peripheral COMT. Tolcapone caused a rapid and reversible inhibition of COMT activity in erythrocytes in parallel with a dose-dependent decrease in the formation of 3-OMD. Tolcapon
4、e increased the area under the concentration-time curve and elimination half-life of levodopa. Tolcapone crosses the blood-brain barrier, and has been used for L-DOPA adjunct therapy in the treatment of Parkinsons disease.REFERENCES1. Neil E. Paterson, Jennifer Ricciardi, Caitlin Wetzler, et al. Sub
5、-optimal performance in the 5-choice serial reaction time task in rats was sensitive to methylphenidate, atomoxetine and d-amphetamine, but unaffected by the COMT inhibitor tolcapone. Neuros2. Saviana Di Giovanni, Simona Eleuteri, Katerina E. Paleologou, et al. Entacapone and Tolcapone, Two Catechol
6、 O-Methyltransferase Inhibitors, Block Fibril Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1Formation of -Synuclein and -Amyloid and Protect against Amyloid-induced Toxicity. The Journal of Bi3. Panos Bitsios, Panos Roussos1. Tolcapone, COMT polymorphisms and pharmacogenomic t
7、reatment of schizophrenia. Pharmacogenomics. 2001,12 (4): 559-566.4. M.A. Vieira-Coelho, P. Soares-da-Silva. Ontogenic aspects of liver and kidney catechol-O- methyltransferase sensitivity to tolcapone. British Journal of Pharmacology.1996,117 (3):516-520.5. J. Dingemanse, K. Jorga, G. Zurcher,et al
8、. Pharmacokinetic-pharmacodynamic interaction between the COMT inhibitor tolcapone and single-dose levodopa. British Journal of Clinical Pharmacology 1995, 40 (3):253-262.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
