| Description | Disufenton sodium (NXY-059), a new-type nitrone, exhibits potently neuroprotective effects. |
| In vitro | NXY-059 is more soluble than the spin trapping agent α-phenyl-N-tert-butyl nitrone (PBN). [1] 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. [2] |
| 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. [1] 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. [3] Treatment with NXY-059 (50 mg/kg subcutaneous plus 8.8 mg/kg/h for 3 days subcutaneous delivered via implanted osmotic pumps) significantly decreases neurological impairment following intracerebral hemorrhage in rat, and reduces the neutrophil infiltrate observed 48 hours post-hemorrhage in the vicinity of the hematoma, and the number of TUNEL-positive cells 48 hours post-hemorrhage at the hematoma margin. [4] |
| Synonyms | Cerovive, NXY059, OKN007, NXY-059, NXY 059 |
| molecular weight | 381.33 |
| Molecular formula | C11H13NNa2O7S2 |
| CAS | 168021-79-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 70 mg/mL (183.6 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 45 mg/mL (118.01 mM) |
| References | 1. Kuroda S, et al, J Cereb Blood Flow Metab, 1999, 19(7), 778-787. 2. Culot M, et al, Brain Res, 2009, 19(1294), 144-152. 3. Marshall JW, et al, Stroke, 2001, 32(1), 190-198. 4. Peeling J, et al, Neuropharmacology, 2001, 40(3), 433-439. |
| Citations | 1. Martínez-Alonso E, Escobar-Peso A, Aliena-Valero A, et al. Preclinical Characterization of Antioxidant Quinolyl Nitrone QN23 as a New Candidate for the Treatment of Ischemic Stroke. Antioxidants. 2022, 11(6): 1186 |