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Opicapone

Catalog No. T16398   CAS 923287-50-7
Synonyms: BIA 9-1067

Opicapone (BIA 9-1067) 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.

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Opicapone Chemical Structure
Opicapone, CAS 923287-50-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 59.00
2 mg In stock $ 86.00
5 mg In stock $ 143.00
10 mg In stock $ 243.00
25 mg In stock $ 446.00
50 mg In stock $ 658.00
100 mg In stock $ 938.00
1 mL * 10 mM (in DMSO) In stock $ 159.00
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Purity: 100%
Purity: 97.39%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Opicapone (BIA 9-1067) 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 decreases the mitochondrial membrane potential of the cells (IC50: 181 μM). Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of L-DOPA, without inducing toxicity. 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) [1].
In vivo Opicapone inhibited rat peripheral COMT with ED50 values below 1.4 mg kg(-1) up to 6 h post-administration.?The effect was 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 levodopa levels with a concomitant reduction in 3-O-methyldopa from 2 h up to 24 h post-administration, while tolcapone produced significant effects only at 2 h post-administration.?The effects of opicapone on brain catecholamines after levodopa administration were sustained up to 24 h post-administration.?Opicapone was 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[1].
Synonyms BIA 9-1067
Molecular Weight 413.17
Formula C15H10Cl2N4O6
CAS No. 923287-50-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (242.03 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Bonifácio MJ, et al. Pharmacological profile of Opicapone, a third-generation nitrocatechol catechol-O-methyl transferase inhibitor, in the rat. Br J Pharmacol. 2015 Apr;172(7):1739-52. 2. Ferreira JJ, et al. Opicapone as an adjunct to L-DOPA in patients with Parkinson's disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial. Lancet Neurol. 2016 Feb;15(2):154-165.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library FDA-Approved & Pharmacopeia Drug Library FDA-Approved Drug Library Metabolism Compound Library Human Metabolite Library ReFRAME Related Library Anti-Metabolism Disease Compound Library

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Keywords

Opicapone 923287-50-7 Metabolism Transferase BIA 9-1067 Inhibitor inhibit COMT inhibitor

 

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