NXY-059

Catalog No.S6002 Synonyms: Cerovive, Disufenton Sodium

NXY-059  Chemical Structure

Molecular Weight(MW): 381.33

NXY-059 is a novel nitrone, shows efficacious neuroprotective effects. Phase 3.

Size Price Stock Quantity  
In DMSO USD 100 In stock
USD 80 In stock
USD 370 In stock

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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
+ Expand
  • Animal Models: Monofilament fishing line is used to produce occlusion and neurologic deficit in male Wistar rats
  • Formulation: NXY-059 is dissolved in physiological saline.
  • Dosages: 0.3, 3.0 or 30 mg/kg
  • Administration: Administered into the right jugular vein.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (199.3 mM)
Water 76 mg/mL (199.3 mM)
Ethanol <1 mg/mL
In vivo Saline 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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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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