GLPBio

NXY-059

Catalog No.: GC13345Purity:>98.00%Synonyms: CPI-22, Disufenton Sodium
NXY-059 is a neuroprotective free radical trapping agent that reduces oxidative damage by neutralizing free radicals, while also mitigating neuroinflammation by protecting the integrity of the blood-brain barrier.

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NXY-059
Cas No.: 168021-79-2
10mM (in 1mL DMSO)In Stock
$34.00
1
5mgIn Stock
$31.00
1
10mgIn Stock
$48.00
1
50mgIn Stock
$152.00
1
100mgIn Stock
$240.00
1

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Description

NXY-059 is a neuroprotective free radical trapping agent that reduces oxidative damage by neutralizing free radicals, while also mitigating neuroinflammation by protecting the integrity of the blood-brain barrier[1-2]. NXY-059 is applicable for research related to acute ischemic stroke[3-4].

In vitro, NXY-059 (250μM) was applied to a co-culture model of bovine brain capillary endothelial cells and glial cells under oxygen-glucose deprivation (OGD) conditions. NXY-059 significantly inhibited the OGD-induced increase in sucrose permeability and reduced the abnormal transcellular transport of tissue-type plasminogen activator (tPA) from the luminal to the brain side [5]. NXY-059 (300μM) pretreated N1E-115 neuroblastoma cells for 30 minutes. NXY-059 failed to inhibit cell death induced by sodium nitroprusside (SNP; 100μM)[6].

In vivo, NXY-059 (3, 10, and 30mg/kg/h) was intravenously infused in a rat model of transient middle cerebral artery occlusion, starting 2.25 hours after occlusion and continuing for 21.75 hours. NXY-059 significantly reduced neurological deficits and histologically measured infarct volume, with the protective effect linearly correlating with plasma concentration[7]. NXY-059 (3 or 10mg/kg) was intravenously administered in a transient focal cerebral ischemia model in Sprague-Dawley rats, with injections at 0 and 30 minutes after occlusion. NXY-059 significantly reduced cortical infarct volume, decreased the number of apoptotic cells, and suppressed ischemia-induced cell death[8].

References:
[1] Fong JJ, Rhoney DH. NXY-059: review of neuroprotective potential for acute stroke. Ann Pharmacother. 2006 Mar;40(3):461-71.
[2] Wang CX, Shuaib A. NXY-059: a neuroprotective agent in acute stroke. Int J Clin Pract. 2004 Oct;58(10):964-9.
[3] Maples KR, Green AR, Floyd RA. Nitrone-related therapeutics: potential of NXY-059 for the treatment of acute ischaemic stroke. CNS Drugs. 2004;18(15):1071-84.
[4] Lees KR, Zivin JA, Ashwood T, et al. NXY-059 for acute ischemic stroke. N Engl J Med. 2006 Feb 9;354(6):588-600.
[5] Culot M, Mysiorek C, Renftel M, et al. Cerebrovascular protection as a possible mechanism for the protective effects of NXY-059 in preclinical models: an in vitro study. Brain Res. 2009 Oct 19;1294:144-52.
[6] Hainsworth AH, Bhuiyan N, Green AR. The nitrone disodium 2,4-sulphophenyl-N-tert-butylnitrone is without cytoprotective effect on sodium nitroprusside-induced cell death in N1E-115 neuroblastoma cells in vitro. J Cereb Blood Flow Metab. 2008 Jan;28(1):24-8.
[7] Sydserff SG, Borelli AR, Green AR, et al. NXY-059 on infarct volume after transient or permanent middle cerebral artery occlusion in the rat; studies on dose, plasma concentration and therapeutic time window. Br J Pharmacol. 2002 Jan;135(1):103-12.
[8] Takizawa S, Izuhara Y, Kitao Y, et al. A novel inhibitor of advanced glycation and endoplasmic reticulum stress reduces infarct volume in rat focal cerebral ischemia. Brain Res. 2007 Dec 5;1183:124-37.

Protocol

Cell experiment [1]:

Cell lines

N1E-115 neuroblastoma cells (mouse neuroblastoma-derived clonal cell line)

Preparation Method

N1E-115 cells were maintained in Dulbecco's modified Eagle medium:Ham F-12 medium supplemented with 10% heat-inactivated fetal bovine serum at 37°C, 5% CO₂. Cells were pretreated with NXY-059 at a concentration known to be neuroprotective in vivo (300μM) for 30 minutes.

Reaction Conditions

300μM; 24 hours

Applications

NXY-059 showed no cytoprotective effect on SNP-induced cell death in N1E-115 neuroblastoma cells. NXY-059 was also without effect on H₂O₂-mediated cytotoxicity. These results suggest that the neuroprotective effects of NXY-059 observed in vivo are not mediated via a direct cytoprotective action on neuronal-type cells.

Animal experiment [2]:

Animal models

Male Wistar Kyoto rats

Preparation Method

Rats were subjected to either transient (2-hour) or permanent occlusion of the middle cerebral artery (MCA). For the transient model, NXY-059 was administered via continuous intravenous infusion (3, 10, and 30mg/kg/h) for 21.75 hours, starting 2.25 hours after occlusion.

Dosage form

3-30mg/kg/h; i.v. infusion; starting 2.25 hours after occlusion for 21.75 hours.

Applications

NXY-059 produced a dose-dependent reduction in infarct volume and neurological impairment in both transient and permanent MCA occlusion models. In the transient model, a dose of 10mg/kg/h decreased in infarct volume.

References:
[1] Hainsworth AH, Bhuiyan N, Green AR. The nitrone disodium 2,4-sulphophenyl-N-tert-butylnitrone is without cytoprotective effect on sodium nitroprusside-induced cell death in N1E-115 neuroblastoma cells in vitro. J Cereb Blood Flow Metab. 2008 Jan;28(1):24-8.
[2] Sydserff SG, Borelli AR, Green AR, et al. NXY-059 on infarct volume after transient or permanent middle cerebral artery occlusion in the rat; studies on dose, plasma concentration and therapeutic time window. Br J Pharmacol. 2002 Jan;135(1):103-12.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
168021-79-2
Synonyms
CPI-22, Disufenton Sodium
Chemical Name
disodium;4-[(Z)-[tert-butyl(oxido)azaniumylidene]methyl]benzene-1,3-disulfonate
SMILES
CC(C)(C)[N+](=CC1=C(C=C(C=C1)S(=O)(=O)[O-])S(=O)(=O)[O-])[O-].[Na+].[Na+]
Molecular Formula
C11H13NNa2O7S2
Molecular Weight
381.33
Solubility
DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 10 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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