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EUK 134

现货
Catalog No.
B1325
Salen-锰复合物; SOD模拟物
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
20mg
¥ 820.00
现货
50mg
¥ 1,380.00
现货

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Background

EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, has exhibited potent antioxidant activities and inhibited the formation of β-amyloid and related amyloid fibril.

In vitro:EUK-134, a salen-manganese complex, showed potent catalase and cytoprotective activities and SOD activity. After middle cerebral artery occlusion, EUK-134 administration at 3 hr significantly reduced brain infarct size, with the highest dose apparently preventing further infarct growth[1]. Administration of EUK 134 (20 μM) prevented Aβ-induced microglial proliferation in vitro[2]. In human neuroblastoma cell line SK-N-MC, pre-treatments with EUK134 protected cells against H2O2-induced oxidative stress through inhibition of MAPK pathway in a dose-dependent manner.EUK134 also decreased the expression of pro-apoptotic genes p53 and Bax and enhanced expression of anti-apoptotic Bcl-2 gene [3]. Incubation of human amylin with EUK-134 significantly inhibited amyloid formation at two molar ratios of 1:1 and 5:1 (drugs to protein)[4].

In vivo:Compared to the vehicle-injected rats, the EUK-134-treated group at doses of 0.5 and 5.0 μmol/kg (0.25 and 2.5 mg/kg, respectively) exhibited infarct volumes that were significantly lower than those of vehicle-injected rats. At 5.0 μmol/kg, EUK-134 reduced the infarct volume by 90% when compared with that of the vehicle controls [1].EUK-134 protected most of the vulnerable neurons from excitotoxic cell death.EUK-134 significantly reduced (P< 0.05) KA-induced neuronal damage in CA1 (22% of total neurons), an almost complete protection in CA3 (7%) and piriform cortex (14%), indicating that EUK-134 prevented most but not all neuronal damage resulting from KA-induced seizure activity [5].

References:
[1].  Baker K, Marcus C B, Huffman K, et al. Synthetic combined superoxide dismutase/catalase mimetics are protective as a delayed treatment in a rat stroke model: a key role for reactive oxygen species in ischemic brain injury[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 284(1): 215-221.
[2].  Jekabsone A, Mander P K, Tickler A, et al. Fibrillar beta-amyloid peptide Aβ 1–40 activates microglial proliferation via stimulating TNF-α release and H 2 O 2 derived from NADPH oxidase: a cell culture study[J]. Journal of neuroinflammation, 2006, 3(1): 1.
[3].  Mohammadi M, Yazdanparast R. Modulation of H2O2‐Induced Mitogen‐Activated Protein Kinases Activation and Cell Death in SK‐N‐MC Cells by EUK134, a SalenDerivative[J]. Basic & clinical pharmacology & toxicology, 2011, 108(6): 378-384.
[4].  Bahramikia S, Yazdanparast R. Inhibition of human islet amyloid polypeptide or amylin aggregation by two manganese-salenderivatives[J]. European journal of pharmacology, 2013, 707(1): 17-25.
[5].  Rong Y, Doctrow S R, Tocco G, et al. EUK-134, a synthetic superoxide dismutase and catalase mimetic, prevents oxidative stress and attenuates kainate-induced neuropathology[J]. Proceedings of the National Academy of Sciences, 1999, 96(17): 9897-9902.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt416.74
Cas No.81065-76-1
FormulaC18H18ClMnN2O4
Solubility≥20.85mg/mL in DMSO
Chemical Namemanganese(2+);2-methoxy-6-[2-[(3-methoxy-2-oxidophenyl)methylideneamino]ethyliminomethyl]phenolate;chloride
SDFDownload SDF
Canonical SMILESCOC1=CC=CC(=C1[O-])C=NCCN=CC2=C(C(=CC=C2)OC)[O-].[Cl-].[Mn+2]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人皮肤成纤维细胞

溶解方法

该化合物在DMSO中的溶解度>20.9mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0, 20, 40, 60和80 μM, 18h

应用

在人类真皮成纤维细胞中,EUK-134具有比EUK-8显著更大的细胞保护活性。EUK-134(80μM)与290单位/ ml牛肝过氧化氢酶具有一样的保护作用。

动物实验[1]:

动物模型

中脑动脉闭塞(MCA-o)的雄性Sprague-Dawley大鼠

剂量

0.25和2.5 mg/kg, 稀释在0.9%盐水中,在MCA-o后3小时单次静脉推注,在21小时或72小时处死。

应用

在中脑动脉闭塞(MCA-o)的雄性Sprague-Dawley大鼠中,与载体注射的大鼠相比,EUK-134显著降低梗死体积。2.5mg / kg的EUK-134将梗死体积减少~90%。72小时后,EUK-134治疗组仍然显示出相当程度的保护作用,并且平均梗塞体积与21小时时没有显著差异。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Baker K, Marcus C B, Huffman K, et al. Synthetic combined superoxide dismutase/catalase mimetics are protective as a delayed treatment in a rat stroke model: a key role for reactive oxygen species in ischemic brain injury[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 284(1): 215-221.

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