EUK 134
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EUK 134是一种合成的超氧化物歧化酶(SOD)/过氧化氢酶模拟物,具有高效抗氧化活性,抑制β-淀粉样蛋白和相关淀粉样蛋白原纤维的形成。
体外实验:EUK-134是salen-锰复合物,具有强的过氧化氢酶和细胞保护活性以及SOD活性。大脑中动脉闭塞后,EUK-134给药3小时显著减少脑梗死面积,最高剂量进一步阻止梗死生长[1]。EUK 134(20 μM)阻止Aβ诱导的小胶质细胞增殖[2]。在人神经母细胞瘤细胞系SK-N-MC中,EUK134预处理以剂量依赖性方式抑制MAPK途径,保护细胞免受H2O2诱导的氧化应激反应。EUK134也降低促凋亡基因p53和Bax的表达,并增强抗凋亡Bcl-2基因的表达[3]。药物与蛋白质摩尔比为1:1和5:1时,EUK-134与人胰岛淀粉样多肽孵育显著抑制了淀粉样蛋白形成[4]。
在体实验:与载体注射的大鼠相比,EUK-134处理组在0.5和5.0 μmol/kg(分别为0.25和2.5 mg/kg)的剂量下使梗塞体积显著低于对照组。与载体对照相比时,浓度为5.0 μmol/kg的EUK-134使梗塞体积减少约90%[1]。EUK-134保护大多数脆弱的神经元免受兴奋性毒性细胞死亡。EUK-134显著减少KA诱导的CA1区(总神经元的22%)神经元损伤,几乎完全保护CA3区(7%)和梨状皮质区(14%)(P < 0.05),表明EUK-134阻止KA诱导的癫痫活动所造成的大部分但不是所有的神经元损伤[5]。
参考文献:
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.
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.
Mohammadi M, Yazdanparast R. Modulation of H2O2‐Induced Mitogen‐Activated Protein Kinases Activation and Cell Death in SK‐N‐MC Cells by EUK134, a Salen Derivative[J]. Basic & clinical pharmacology & toxicology, 2011, 108(6): 378-384.
Bahramikia S, Yazdanparast R. Inhibition of human islet amyloid polypeptide or amylin aggregation by two manganese-salen derivatives[J]. European journal of pharmacology, 2013, 707(1): 17-25.
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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 416.74 |
Cas No. | 81065-76-1 |
Formula | C18H18ClMnN2O4 |
Solubility | ≥2.11 mg/mL in H2O; ≥20.85 mg/mL in DMSO; ≥3.24 mg/mL in EtOH |
Chemical Name | manganese(2+);2-methoxy-6-[2-[(3-methoxy-2-oxidophenyl)methylideneamino]ethyliminomethyl]phenolate;chloride |
SDF | Download SDF |
Canonical SMILES | COC1=CC=CC(=C1[O-])C=NCCN=CC2=C(C(=CC=C2)OC)[O-].[Cl-].[Mn+2] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
- 批次: