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.
Cited by 1 publication
Purity & Quality Control
Biological Activity
| Description | NXY-059 is a novel nitrone, shows efficacious neuroprotective effects. Phase 3. |
|---|---|
| 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] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 76 mg/mL (199.3 mM) |
|---|---|---|
| Water | 76 mg/mL (199.3 mM) | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): Saline For best results, use promptly after mixing. |
30 mg/mL |
* 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.
Chemical Information
| Molecular Weight | 381.33 |
|---|---|
| Formula | C11H13NNa2O7S2 |
| CAS No. | 168021-79-2 |
| Storage | powder |
| in solvent | |
| Synonyms | Cerovive, Disufenton Sodium |
Bio Calculators
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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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