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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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| APO866
APO866 is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; NAMPT) with an IC50 of 0.09 nM. |
| Lonafarnib
Lonafarnib (SCH 66336) is a selectively FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. |
| Tolcapone
Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
| Tunicamycin
Tunicamycin is a mixture of nucleoside antibiotics that inhibits N-glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin can cause the accumulation of unfolded proteins within the endoplasmic reticulum (ER) and induce ER stress, leading to impaired DNA synthesis and G1 phase cell cycle arrest. |
| Sandoz 58-035
Sandoz 58-035 is a cholesterol acyltransferase (ACAT) inhibitor. Sandoz 58-035 inhibits the accumulation of cholesteryl esters and inhibits the esterification of cholesterol by 95% in arterial smooth muscle cells in culture. Sandoz 58-035 was used to induce simultaneous activation of unfolded protein response (UPR) and pattern recognition receptors (PRRs) in mouse peritoneal macrophages. |
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