Free shipping on all orders over $ 500

Opicapone

Cat. No. M10100
Opicapone Structure
Synonym:

BIA 9-1067

Size Price Availability Quantity
10mg USD 320  USD320 In stock
25mg USD 555  USD555 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Joaquim J Ferreira, et al. Lancet Neurol. Opicapone as an adjunct to levodopa in patients with Parkinson's disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial

[2] M J Bonifacio, et al. Br J Pharmacol. Pharmacological profile of opicapone, a third-generation nitrocatechol catechol-O-methyl transferase inhibitor, in the rat

Related Transferase Products
Ibiglustat

Ibiglustat (Venglustat) is a potent and selective Glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor.

3-Methoxybenzamide

3-Methoxybenzamide (3-MBA) is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT).

Adenosine Dialdehyde

Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.

Hecogenin

Hecogenin is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM.

OSMI-1

OSMI-1 is a cell permeable inhibitor of OGT (O-GlcNAc transferase) with an IC50 value of 2.7 μM.

  Catalog
Abmole Inhibitor Catalog




Keywords: Opicapone, BIA 9-1067 supplier, Transferase, inhibitors, activators

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.