NXY-059
(Synonyms: 4-[[(1,1-二甲基乙基)氧化亚氨基]甲基]-1,3-苯二磺酸二钠,NXY-059) 目录号 : GC13345
NXY-059具有神经保护活性的自由基捕获剂，NXY-059可中和自由基来减少氧化损伤，同时通过保护血脑屏障完整性以减轻神经炎症。
Cas No.:168021-79-2
Sample solution is provided at 25 µL, 10mM.
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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.
NXY-059具有神经保护活性的自由基捕获剂，NXY-059可中和自由基来减少氧化损伤，同时通过保护血脑屏障完整性以减轻神经炎症[1-2]。NXY-059可用于急性缺血性中风的相关研究[3-4]。
在体外，NXY-059（250μM）在氧糖剥夺（OGD）条件下作用于牛脑毛细血管内皮细胞与胶质细胞共培养模型时，NXY-059显著抑制OGD诱导的蔗糖通透性增加，并降低组织型纤溶酶原激活剂（tPA）从管腔侧向脑侧的异常转运 [5]。NXY-059（300μM）预处理N1E-115神经母细胞瘤细胞30分钟，NXY-059未能抑制由硝普钠（SNP；100μM）诱导的细胞死亡 [6]。
在体内，NXY-059（3，10和30mg/kg/h）静脉输注大鼠短暂性大脑中动脉闭塞模型，从闭塞后2.25小时开始给药持续21.75小时，NXY-059显著减少神经功能缺损和组织学测量的梗死体积，且保护作用与血浆浓度线性相关[7]。NXY-059（3或10mg/kg）静脉注射短暂性局灶性缺血SD大鼠中，分别在闭塞后0和30分钟给药，NXY-059显著降低皮质梗死体积，并减少凋亡细胞数量，抑制缺血诱导的细胞死亡[8]。
| 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: | |
| Cas No. | 168021-79-2 | SDF | |
| 别名 | 4-[[(1,1-二甲基乙基)氧化亚氨基]甲基]-1,3-苯二磺酸二钠,NXY-059 | ||
| 化学名 | disodium;4-[(Z)-[tert-butyl(oxido)azaniumylidene]methyl]benzene-1,3-disulfonate | ||
| Canonical SMILES | CC(C)(C)[N+](=CC1=C(C=C(C=C1)S(=O)(=O)[O-])S(=O)(=O)[O-])[O-].[Na+].[Na+] | ||
| 分子式 | C11H13NNa2O7S2 | 分子量 | 381.33 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6224 mL | 13.112 mL | 26.224 mL |
| 5 mM | 524.5 μL | 2.6224 mL | 5.2448 mL |
| 10 mM | 262.2 μL | 1.3112 mL | 2.6224 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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