NXY-059 (Disufenton sodium)
Catalog No.S6002 Synonyms: Cerovive, Disufenton Sodium
Molecular Weight(MW): 381.33
NXY-059 is a novel nitrone, shows efficacious neuroprotective effects. Phase 3.
Purity & Quality Control
|Description||NXY-059 is a novel nitrone, shows efficacious neuroprotective effects. Phase 3.|
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.  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. |
|In vitro||DMSO||76 mg/mL (199.3 mM)|
|Water||76 mg/mL (199.3 mM)|
|Ethanol||slightly soluble or insoluble|
|In vivo||Add solvents individually and in order:
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Cerovive, Disufenton Sodium|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00075959||Completed||Intracerebral Hemorrhage||AstraZeneca||August 2004||Phase 2|
|NCT00119626||Completed||Cerebral Stroke|Ischemic Attack, Transient||AstraZeneca||June 2003||Phase 3|
|NCT00061022||Completed||Cerebral Stroke|Stroke, Acute|Cerebrovascular Stroke|Ischemic Attack, Transient||AstraZeneca||May 2003||Phase 3|
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