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Opicapone

CAT: 0013-GTR19154758-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19154758-01Size:200 mg
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Description
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.
CAS Number
923287-50-7
Product Name Alternative
BIA 9-1067
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO:100 mg/mL (242.03 mM; Need ultrasonic)
Smiles
OC1=CC (C2=NC (C3=C (Cl) [N+] ([O-]) =C (C) C (Cl) =C3C) =NO2) =CC ([N+] ([O-]) =O) =C1O
Molecular Formula
C15H10Cl2N4O6
Molecular Weight
413.17
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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