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[CAS NO. 923287-50-7] Opicapone
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14896 |
| Brand: | MCE |
| CAS: | 923287-50-7 |
Overview
| MDL | MFCD19443745 |
|---|---|
| Molecular Weight | 413.17 |
| Molecular 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 |
2 Publications Citing Use of MCE
Summary
IC50 & Target
COMT [1]
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 IC 50 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 λ ex 544 λ em 590 over λ ex 485 λ em 538). Opicapone decreases the mitochondrial membrane potential of the cells with IC 50 of 181 μM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Opicapone inhibits rat peripheral COMT with ED 50 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02305017 | Bial - Portela C S.A. |
Parkinson´s Disease
|
March 2014 | Phase 1 |
| NCT01533116 | Bial - Portela C S.A. |
Parkinson Disease
|
March 2009 | Phase 1 |
| NCT02169440 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
June 2009 | Phase 1 |
| NCT02847442 | Bial - Portela C S.A. |
Parkinson´s Disease With Wearing-off Motor Fluctuations
|
November 23, 2016 | Phase 4 |
| NCT01532141 | Bial - Portela C S.A. |
Parkinson Disease
|
November 2009 | Phase 1 |
| NCT03116295 | Bial - Portela C S.A. |
Parkinson Disease
|
June 20, 2017 | Phase 1 |
| NCT01568047 | Bial - Portela C S.A. |
Parkinson´s Disease
|
February 2010 | Phase 2 |
| NCT04986982 | Bial - Portela C S.A. |
Parkinson Disease
|
February 25, 2021 | Phase 4 |
| NCT01851850 | Rabin Medical Center |
Parkinson Disease
|
May 2013 | Phase 3 |
| NCT02170376 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
September 2011 | Phase 1 |
| NCT01515891 | Bial - Portela C S.A. |
Parkinson Disease
|
May 2009 | Phase 1 |
| NCT03820037 | Bial - Portela C S.A. |
Parkinson Disease
|
March 19, 2019 | Phase 1 |
| NCT02169466 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
January 2009 | Phase 1 |
| NCT02071810 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
April 2008 | Phase 1 |
| NCT03959540 | Bial - Portela C S.A. |
Parkinson Disease
|
April 28, 2020 | |
| NCT02101190 | Bial - Portela C S.A. |
Parkinson´s Disease
|
March 2010 | Phase 1 |
| NCT01568073 | Bial - Portela C S.A. |
Parkinson´s Disease
|
March 2011 | Phase 3 |
| NCT01568034 | Bial - Portela C S.A. |
Parkinson´s Disease
|
April 2009 | Phase 2 |
| NCT02305277 | Bial - Portela C S.A. |
Parkinson
|
March 2014 | Phase 1 |
| NCT02305329 | Bial - Portela C S.A. |
Epilepsy
|
February 2014 | Phase 1 |
| NCT02305316 | Bial - Portela C S.A. |
Parkinson Disease
|
February 2014 | Phase 1 |
| NCT02169479 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
September 2008 | Phase 1 |
| NCT02169414 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
February 2010 | Phase 1 |
| NCT04986995 | Bial - Portela C S.A. |
Parkinson Disease
|
June 9, 2021 | Phase 4 |
| NCT01519284 | Bial - Portela C S.A. |
Parkinson Disease
|
November 2009 | Phase 1 |
| NCT01532115 | Bial - Portela C S.A. |
Parkinson Disease
|
May 2010 | Phase 1 |
| NCT01227655 | Bial - Portela C S.A. |
Parkinson´s Disease
|
March 2011 | Phase 3 |
| NCT01532128 | Bial - Portela C S.A. |
Parkinson Disease
|
November 2009 | Phase 1 |
| NCT01520987 | Bial - Portela C S.A. |
Parkinson Disease
|
May 2011 | Phase 1 |
| NCT02071823 | Bial - Portela C S.A. |
Parkinson
|
May 2008 | Phase 1 |
| NCT01533077 | Bial - Portela C S.A. |
Parkinson Disease
|
March 2009 | Phase 1 |
| NCT02305030 | Bial - Portela C S.A. |
Parkinson´s Disease
|
March 2014 | Phase 1 |
| NCT04787965 | Neurocrine Biosciences |
Parkinson Disease
|
March 1, 2021 | |
| NCT02169895 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
September 2008 | Phase 1 |
| NCT04978597 | Bial - Portela C S.A. |
Parkinson
|
May 31, 2021 | Phase 3 |
| NCT03496870 | Neurocrine Biosciences |
Parkinson Disease
|
February 8, 2018 | Phase 1 |
| NCT02169453 | Bial - Portela C S.A. |
Parkinson´s Disease (PD)
|
October 2008 | Phase 1 |
| NCT01520727 | Bial - Portela C S.A. |
Parkinson Disease
|
October 2007 | Phase 1 |
| NCT03116308 | Bial - Portela C S.A. |
Parkinson Disease
|
November 21, 2014 | Phase 1 |
| NCT04990284 | Bial - Portela C S.A. |
Parkinson Disease
|
November 29, 2021 | Phase 4 |
| NCT01536366 | Bial - Portela C S.A. |
Parkinson Disease
|
June 2009 | Phase 1 |
| NCT02092168 | Bial - Portela C S.A. |
Parkinson Disease
|
October 2008 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 242.03 mM ; Need ultrasonic)
H 2 O : < 0.1 mg/mL (insoluble)
Stock Solutions
| Concentration Solvent 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.05 mM); Suspended solution; Need ultrasonic
References
- [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.
Synonyms
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