Tolcapone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种选择性、有效、可逆的硝基儿茶酚型儿茶酚-O-甲基转移酶 (COMT) 抑制剂，用于治疗帕金森病。

A selective, potent and reversible nitrocatechol-type inhibitor of catechol-O-methyltransferase (COMT) for treatment of Parkinson's disease; also kills neuroblastoma (NB) cells in preclinical models by inhibition of COMT; induces oxidative stress leading to apoptosis and inhibition of tumor growth in Neuroblastoma; also is a potent Transthyretin (TTR) aggregation inhibitor.Parkinson's Disease Approved(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.Tolcapone (25, 50,75, 100 μM) treatment activates downstream apoptotic events in NB cells. Tolcapone induces caspase-mediated apoptosis in neuroblastoma.(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.

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.?Tolcapone (25, 50,75, 100 μM) treatment activates downstream apoptotic events in NB cells. Tolcapone induces caspase-mediated apoptosis in neuroblastoma. Cell Viability Assay 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 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.

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. Animal Model:4-week-old female nude mice (nu/nu) bearing SMS‐KCNR xenograft models 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.

Ro 40-7592

Metabolic Enzyme/Protease

COMT

COMT

Neurological Disease

Parkinson Disease

134308-13-7

273.2408

C14H11NO5

>98% (HPLC)

10 mM in DMSO

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

Methanone, (3,4-dihydroxy-5-nitrophenyl)(4-methylphenyl)-

(-20℃)

With Ice Pack

≥ 2 years