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Opicapone

Cat. No. M10100
Opicapone Structure
Synonym:

BIA 9-1067

Size Price Availability Quantity
10mg USD 320  USD320 In stock
25mg USD 555  USD555 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Opicapone, also known as BIA 9-1067, is a novel potent and selective catechol-O-methyltransferase inhibitor (COMT inhibitor). Opicapone provides a superior response upon the bioavailability of levodopa associated to more pronounced, long-lasting, and sustained COMT inhibition. 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). 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 413.17
Formula C15H10Cl2N4O6
CAS Number 923287-50-7
Purity >99%
Solubility DMSO 85 mg/mL
Storage at -20°C
References

[1] Joaquim J Ferreira, et al. Lancet Neurol. Opicapone as an adjunct to levodopa in patients with Parkinson's disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial

[2] M J Bonifacio, et al. Br J Pharmacol. Pharmacological profile of opicapone, a third-generation nitrocatechol catechol-O-methyl transferase inhibitor, in the rat

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Opicapone, BIA 9-1067 supplier, Transferase, inhibitors

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