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阿洛司他丁酸

    
10mM in DMSO

E-64c

源叶(MedMol)
T99181 一键复制产品信息
76684-89-4
C15H26N2O5
314.38
(2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane;(2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T99181-1ml促销
10mM in DMSO

¥516.00 ¥464.00

5 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: E-64衍生物。不可逆半胱氨酸蛋白酶抑制剂。;E-64 ( ab141418 ) derivative. Irreversible cysteine protease inhibitor.;Cysteine protease inhibitor; membrane-impermeable calpain inhibitor. Significantly reduces calpain-mediated depletion of microtubule-associated protein (MAP2) in an animal model of an ischemic brain.;Cysteine protease inhibitor; membrane-impermeable calpain inhibitor. Significantly reduces calpain-mediated depletion of microtubule-associated protein (MAP2) in an animal model of an ischemic brain.
靶点: Cysteine proteases, CANP, Cathepsin C.
体内研究: The t-1/2 of plasma E-64c is 0.48 hours. The hemodynamic effects of E-64c are absent at this dose. Using two way analysis of variance, the effects of reperfusion (p=0.0016) or E-64c (p=0.0226) per se on infarct size are significant. In comparing Group A with Group B and Group C with Group D, the depletion of CPK in the E-64c treated groups (Groups A and C) is slightly less than in the vehicle-injected groups (Groups B and D). The insufficient effect of E-64c alone may be explained by the early administration and relatively short t-1/2. Since the effectiveness of NCO-700 has been established,6),7) our findings might indicate a small but beneficial effect of E-64c on infarct size and CPK content.
参考文献: 1. Khan MS, et al. Design, synthesis, evaluation and thermodynamics of 1-substituted pyridylimidazo[1,5-a]pyridine derivatives as cysteine protease inhibitors. PLoS One. 2013 Aug 5;8(8):e69982.
2. Toda G, et al. Calcium-activated neutral protease inhibitor (E-64c) and reperfusion for experimental myocardial infarction. Jpn Heart J. 1989 May;30(3):375-86.
3. Radzey H, et al. E-64c-hydrazide: a lead structure for the development of irreversible cathepsin C inhibitors. ChemMedChem. 2013 Aug;8(8):1314-21.
4. Ji Yeun Kim, et al. Safe, High-Throughput Screening of Natural Compounds of MERS-CoV Entry Inhibitors Using a Pseudovirus Expressing MERS-CoV Spike Protein. Int J Antimicrob Agents. 2018 Nov;52(5):730-732.
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.181 ml 15.904 ml 31.809 ml
5 mM 0.636 ml 3.181 ml 6.362 ml
10 mM 0.318 ml 1.59 ml 3.181 ml
50 mM 0.064 ml 0.318 ml 0.636 ml
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参考文献

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摩尔浓度计算器

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