Opicapone

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

Opicapone 降低细胞的 ATP 含量（IC50：98 μM）。

Opicapone reduces the ATP content of the cells (IC50: 98 μM). Opicapone is an effective third-generation catechol-O-methyltransferase inhibitor for the research of Parkinson's disease and motor fluctuations. (In Vitro):Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of L-DOPA, without inducing toxicity. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM. Incubation of human primary hepatocytes for 24 h with increasing concentrations of Ro 40-7592, OR-611 or Opicapone resulted in a concentration-dependent decrease in the mitochondrial membrane potential of the cells, evaluated by the ratio JC-1 aggregates over JC-1 monomer (ratio λex 544 λem 590 over λex 485 λem 538). Opicapone decreases the mitochondrial membrane potential of the cells with IC50 of 181 μM.(In Vivo):Opicapone inhibits rat peripheral COMT with ED50 values below 1.4 mg/kg up to 6 h post-administration. The effect is sustained over the first 8 h and by 24 h COMT had not returned to control values. A single administration of Opicapone resulted in increased and sustained plasma L-DOPA levels with a concomitant reduction in 3-OMD from 2 h up to 24 h post-administration, while Ro 40-7592 produces significant effects only at 2 h post-administration. The effects of Opicapone on brain catecholamines after L-DOPA administration are sustained up to 24 h post-administration. Opicapone is also the least potent compound in decreasing both the mitochondrial membrane potential and the ATP content in human primary hepatocytes after a 24 h incubation period.

Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of L-DOPA, without inducing toxicity. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM. Incubation of human primary hepatocytes for 24 h with increasing concentrations of Ro 40-7592, OR-611 or Opicapone resulted in a concentration-dependent decrease in the mitochondrial membrane potential of the cells, evaluated by the ratio JC-1 aggregates over JC-1 monomer (ratio λex 544 λem 590 over λex 485 λem 538). Opicapone decreases the mitochondrial membrane potential of the cells with IC50 of 181 μM.

Opicapone inhibits rat peripheral COMT with ED50 values below 1.4 mg/kg up to 6 h post-administration. The effect is sustained over the first 8 h and by 24 h COMT had not returned to control values. A single administration of Opicapone resulted in increased and sustained plasma L-DOPA levels with a concomitant reduction in 3-OMD from 2 h up to 24 h post-administration, while Ro 40-7592 produces significant effects only at 2 h post-administration. The effects of Opicapone on brain catecholamines after L-DOPA administration are sustained up to 24 h post-administration. Opicapone is also the least potent compound in decreasing both the mitochondrial membrane potential and the ATP content in human primary hepatocytes after a 24 h incubation period.

BIA 9-1067

Metabolic Enzyme/Protease

Transferase

COMT

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923287-50-7

413.17

C15H10Cl2N4O6

>98% (HPLC)

DMSO:100 mg/mL (242.03 mM; Need ultrasonic)

OC1=CC(C2=NC(C3=C(Cl)[N+]([O-])=C(C)C(Cl)=C3C)=NO2)=CC([N+]([O-])=O)=C1O

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(-20℃)

With Ice Pack

≥ 2 years