1. Metabolic Enzyme/Protease
    Neuronal Signaling
  2. COMT

Opicapone (Synonyms: BIA 9-1067)

Cat. No.: HY-14896
Handling Instructions

Opicapone is an available catechol-O-methyltransferase (COMT) inhibitor. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM.

For research use only. We do not sell to patients.
Opicapone Chemical Structure

Opicapone Chemical Structure

CAS No. : 923287-50-7

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  • Biological Activity

  • Protocol

  • Technical Information

  • References

Description

Opicapone is an available catechol-O-methyltransferase (COMT) inhibitor. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM.

IC50 & Target

COMT[1]

In Vitro

Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of levodopa, 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 Tolcapone, entacapone 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[1].

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 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 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[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01515891 Bial - Portela C S.A. Parkinson Disease May 2009 Phase 1
NCT02101190 Bial - Portela C S.A. Parkinson's Disease March 2010 Phase 1
NCT02092168 Bial - Portela C S.A. Parkinson Disease October 2008 Phase 1
NCT02169440 Bial - Portela C S.A. Parkinson's Disease (PD) June 2009 Phase 1
NCT01536366 Bial - Portela C S.A. Parkinson Disease June 2009 Phase 1
NCT01532141 Bial - Portela C S.A. Parkinson Disease November 2009 Phase 1
NCT01533077 Bial - Portela C S.A. Parkinson Disease March 2009 Phase 1
NCT02071823 Bial - Portela C S.A. Parkinson May 2008 Phase 1
NCT01520727 Bial - Portela C S.A. Parkinson Disease October 2007 Phase 1
NCT01532128 Bial - Portela C S.A. Parkinson Disease November 2009 Phase 1
NCT01520987 Bial - Portela C S.A. Parkinson Disease May 2011 Phase 1
NCT02071810 Bial - Portela C S.A. Parkinson's Disease (PD) April 2008 Phase 1
NCT01227655 Bial - Portela C S.A. Parkinson's Disease March 2011 Phase 3
NCT01532115 Bial - Portela C S.A. Parkinson Disease May 2010 Phase 1
NCT01533116 Bial - Portela C S.A. Parkinson Disease March 2009 Phase 1
NCT02169466 Bial - Portela C S.A. Parkinson's Disease (PD) January 2009 Phase 1
NCT02169453 Bial - Portela C S.A. Parkinson's Disease (PD) October 2008 Phase 1
NCT01568073 Bial - Portela C S.A. Parkinson's Disease March 2011 Phase 3
NCT02169414 Bial - Portela C S.A. Parkinson's Disease (PD) February 2010 Phase 1
NCT01519284 Bial - Portela C S.A. Parkinson Disease November 2009 Phase 1
NCT02170376 Bial - Portela C S.A. Parkinson's Disease (PD) September 2011 Phase 1
NCT02169895 Bial - Portela C S.A. Parkinson's Disease (PD) September 2008 Phase 1
NCT02169479 Bial - Portela C S.A. Parkinson's Disease (PD) September 2008 Phase 1
NCT01568034 Bial - Portela C S.A. Parkinson's Disease April 2009 Phase 2
NCT02305030 Bial - Portela C S.A. Parkinson's Disease March 2014 Phase 1
NCT02847442 Bial - Portela C S.A. Parkinson's Disease With Wearing-off Motor Fluctuations November 23, 2016 Phase 4
NCT03119194 Bial - Portela C S.A. Parkinson Disease February 10, 2017 Phase 1
NCT02305316 Bial - Portela C S.A. Parkinson Disease February 2014 Phase 1
NCT02305277 Bial - Portela C S.A. Parkinson March 2014 Phase 1
NCT02305329 Bial - Portela C S.A. Epilepsy February 2014 Phase 1
NCT02305017 Bial - Portela C S.A. Parkinson's Disease March 2014 Phase 1
NCT01568047 Bial - Portela C S.A. Parkinson's Disease February 2010 Phase 2
NCT01515891 Bial - Portela C S.A. Parkinson Disease May 2009 Phase 1
NCT02101190 Bial - Portela C S.A. Parkinson's Disease March 2010 Phase 1
NCT02092168 Bial - Portela C S.A. Parkinson Disease October 2008 Phase 1
NCT02169440 Bial - Portela C S.A. Parkinson's Disease (PD) June 2009 Phase 1
NCT01536366 Bial - Portela C S.A. Parkinson Disease June 2009 Phase 1
NCT01532141 Bial - Portela C S.A. Parkinson Disease November 2009 Phase 1
NCT01533077 Bial - Portela C S.A. Parkinson Disease March 2009 Phase 1
NCT02071823 Bial - Portela C S.A. Parkinson May 2008 Phase 1
NCT01520727 Bial - Portela C S.A. Parkinson Disease October 2007 Phase 1
NCT01532128 Bial - Portela C S.A. Parkinson Disease November 2009 Phase 1
NCT01520987 Bial - Portela C S.A. Parkinson Disease May 2011 Phase 1
NCT02071810 Bial - Portela C S.A. Parkinson's Disease (PD) April 2008 Phase 1
NCT01227655 Bial - Portela C S.A. Parkinson's Disease March 2011 Phase 3
NCT01532115 Bial - Portela C S.A. Parkinson Disease May 2010 Phase 1
NCT01533116 Bial - Portela C S.A. Parkinson Disease March 2009 Phase 1
NCT02169466 Bial - Portela C S.A. Parkinson's Disease (PD) January 2009 Phase 1
NCT02169453 Bial - Portela C S.A. Parkinson's Disease (PD) October 2008 Phase 1
NCT01568073 Bial - Portela C S.A. Parkinson's Disease March 2011 Phase 3
NCT02169414 Bial - Portela C S.A. Parkinson's Disease (PD) February 2010 Phase 1
NCT01519284 Bial - Portela C S.A. Parkinson Disease November 2009 Phase 1
NCT02170376 Bial - Portela C S.A. Parkinson's Disease (PD) September 2011 Phase 1
NCT02169895 Bial - Portela C S.A. Parkinson's Disease (PD) September 2008 Phase 1
NCT02169479 Bial - Portela C S.A. Parkinson's Disease (PD) September 2008 Phase 1
NCT01568034 Bial - Portela C S.A. Parkinson's Disease April 2009 Phase 2
NCT02305030 Bial - Portela C S.A. Parkinson's Disease March 2014 Phase 1
NCT02847442 Bial - Portela C S.A. Parkinson's Disease With Wearing-off Motor Fluctuations November 23, 2016 Phase 4
NCT03119194 Bial - Portela C S.A. Parkinson Disease February 10, 2017 Phase 1
NCT02305316 Bial - Portela C S.A. Parkinson Disease February 2014 Phase 1
NCT02305277 Bial - Portela C S.A. Parkinson March 2014 Phase 1
NCT02305329 Bial - Portela C S.A. Epilepsy February 2014 Phase 1
NCT02305017 Bial - Portela C S.A. Parkinson's Disease March 2014 Phase 1
NCT01568047 Bial - Portela C S.A. Parkinson's Disease February 2010 Phase 2
NCT03116308 Bial - Portela C S.A. Parkinson Disease November 21, 2014 Phase 1
NCT03116295 Bial - Portela C S.A. Parkinson Disease June 21, 2017 Phase 1
NCT01851850 Rabin Medical Center Parkinson Disease May 2013 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.4203 mL 12.1016 mL 24.2031 mL
5 mM 0.4841 mL 2.4203 mL 4.8406 mL
10 mM 0.2420 mL 1.2102 mL 2.4203 mL
Kinase Assay
[1]

ATP content of human primary hepatocytes is determined using the ATP Lite assay system, which is based on the production of light caused by the reaction of ATP with added luciferase and D-luciferin. Twenty-four hours after being seeded, cell cultures are washed with Hank's balanced salt solution (HBSS) and are then incubated with test compounds prepared in culture media without fetal bovine serum (0, 1.56, 3.13, 6.25, 12.5, 25, 50, 100 and 200 μM) for 24 h at 37°C in humidified 5% CO2-95% air. Positive controls (cells incubated with carbonyl cyanide-p-trifluoromethoxyphenylhydrazone-FCCP, 10 and 50 μM) are run in parallel. After incubation, media are removed from the wells and substituted with 100 μL HBSS plus 50 μL cell lysis solution. Plates are shaken for 5 min at 400 r.p.m. at room temperature. Substrate solution (50 μL) is then added to each well and plates are again shook for 5 min at 400 r.p.m. at room temperature in subdued light. Three standard concentrations of ATP (1, 10 and 100 μM) and blanks are run in parallel in plate wells without cells. Plates are dark adapted for 10 min and luminescence is determined on a MicrobetaTriLux scintillation counter[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Opicapone is prepared in 0.5% carboxymethylcellulose[1].

Rat[1]
Male Wistar rats (240) are used. In experiments designed to evaluate the efficacy of the compound at inhibiting COMT, animals are administered Opicapone (0.03, 0.1, 0.3, 0.6, 1, 3 and 10 mg/kg) and are killed at 2 and 6 h post-administration. In experiments designed to evaluate COMT time-activity profile, animals are given Opicapone (3 mg/kg) and are killed at different post-administration periods (15 and 30 min, and 1, 2, 4, 8, 18, 24, and 48 h). In experiments designed to evaluate the effects of the compounds on central catecholamines, animals are given 3 mg/kg Opicapone or Tolcapone and 1 h before being killed, animals are administered levodopa/benserazide (levodopa 12 mg/kg and benserazide 3 mg/kg). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

413.17

Formula

C₁₅H₁₀Cl₂N₄O₆

CAS No.

923287-50-7

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 1.25 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Opicapone
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