NXY-059

Catalog No.S6002

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

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NXY-059  Chemical Structure

NXY-059 Chemical Structure
Molecular Weight: 381.33

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

NXY-059 is available in the following compound libraries:

Product Information

Product Description

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]
Features

Protocol(Only for Reference)

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

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.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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

Chemical Information

Download NXY-059 SDF
Molecular Weight (MW) 381.33
Formula

C11H13NNa2O7S2

CAS No. 168021-79-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms Cerovive, Disufenton Sodium
Solubility (25°C) * In vitro DMSO 76 mg/mL (199.3 mM)
Water 76 mg/mL (199.3 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name 1,3-Benzenedisulfonic acid, 4-[[(1,1-dimethylethyl)imino]methyl]-, N-oxide, disodium salt

Tech Support

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