[CAS NO. 923287-50-7] Opicapone

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PRODUCTS SPECIFICATIONS [923287-50-7]

Catalog

HY-14896

Brand

MCE

CAS

923287-50-7

DESCRIPTION [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

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Opicapone (BIA 9-1067) is a potent third-generation catechol-O-methyltransferase ( COMT ) inhibitor for the research of Parkinson's disease and motor fluctuations. Opicapone decreases the ATP content of the cells with an IC ₅₀ of 98 μM ^[1] .

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

In Vitro:

DMSO : 100 mg/mL ( 242.03 mM ; Need ultrasonic)

H ₂ O : < 0.1 mg/mL (insoluble)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

Synonyms

1,2-Benzenediol, 5-[3-(2,5-dichloro-4,6-dimethyl-1-oxido-3-pyridinyl)-1,2,4-oxadiazol-5-yl]-3-nitro-

5-[3-(2,5-Dichloro-4,6-dimethyl-1-oxido-3-pyridinyl)-1,2,4-oxadiazol-5-yl]-3-nitro-1,2-benzenediol

Opicapone

BIA 9-1067

5-[3-(2,5-Dichloro-4,6-dimethyl-1-oxy-pyridin-3-yl)-[1,2,4]oxadiazol-5-yl]-3-nitrobenzene-1,2-diol

Ongentys

2,5-Dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine 1-oxide