Brief Description

NXY-059 (Cerovive) is the disulfonyl derivative of the neuroprotective spin trap phenylbutynitrone(PBN), both NXY-059, its parent PBN and their hydrolysis/oxidation product MNT are very powerful scavengers of free radicals.
Target: Neuroprotectant
in vitro: NXY-059 is more soluble than the spin trapping agent α-phenyl-N-tert-butyl nitrone (PBN). In an in vitro blood-brain barrier (BBB) model, 250 mM of NXY-059 administered at the onset or up to 4 h after oxygen glucose deprivation (OGD) produces a significant reduction in the increased BBB permeability caused by OGD. Furthermore, OGD produces a huge influx of tissue plasminogen activator across the BBB, which is substantially reduced by NXY-059.
in vivo: NXY-059 reduces infarct volume in rats subjected to 2 hours of middle cerebral artery occlusion in a dose-dependent manner. At equimolar doses (3.0 mg/kg for NXY-059 and 1.4 mg/kg for PBN), NXY-059 is more efficacious than PBN. Similar results are obtained when a recovery period of 7 days is allowed. The window of therapeutic opportunity for NXY-059 is 3 to 6 hours after the start of recirculation. NXY-059, a free radical-trapping agent, has a substantial protective effect, lessening the disability caused by an experimentally induced stroke in a primate species. NXY-059 treatment reduces the overall amount of brain damage by >50% of saline-treatment values, with similar levels of protection afforded to both white and gray matter.

Solubility

DMSO ≥74mg/mL, Water ≥74mg/mL, Ethanol ≥1.6mg/mL

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid