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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.
| Molecular Weight | 413.17 |
| Formula | C15H10Cl2N4O6 |
| CAS Number | 923287-50-7 |
| Solubility (25°C) | DMSO 85 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Transferase Products |
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| P053
P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5 μM. P053 also acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. |
| ABT-046
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1. |
| JTP-103237
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| PF-06424439
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Products are for research use only. Not for human use. We do not sell to patients.
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