Opicapone, Inhibitor

Opicapone

Cat. Num. AAA5755308

• Purity: 98.00%
• Synonyms: Opicapone; BIA 9-1067; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (242.03mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C15H10Cl2N4O6
• SMILES: CC1=[N+]([O-])C(Cl)=C(C2=NOC(C3=CC([N+]([O-])=O)=C(O)C(O)=C3)=N2)C(C)=C1Cl
• CAS Number: 923287-50-7
• Target & IC50: COMT
• In Vitro: 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 hours incubation period. Opicapone inhibits rat peripheral COMT with ED50 values below 1.4mg/kg up to 6 h post-administration. The effect is sustained over the first 8 h and by 24 hours COMT had not returned to control values. Opicapone (a single administration) resulted in increased and sustained plasma L-DOPA levels with a concomitant reduction in 3-OMD from 2 hours up to 24 hour post-administration, while Ro 40-7592 produces significant effects only at 2 hour post-administration. The effects of Opicapone on brain catecholamines after L-DOPA administration are sustained up to 24 hour post-administration [1].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Opicapone, inhibitor

Opicapone reduces the ATP content of the cells (IC50: 98 uM). Opicapone is an effective third-generation catechol-O-methyltransferase inhibitor for the research of Parkinson's disease and motor fluctuations.

Product Categories/Family for Opicapone, inhibitor

Metabolism; Transferase

References

Bonifacio 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.
Bonifacio 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.
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.
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.