产品属性：
产品名称 | 规格 | CAS号 | 型号 |
MDL 28170 | 10mM (in 1mL DMSO) 10mg 25mg | 88191-84-8 | EY-Y0164954 |
Cas No.88191-84-8
别名 N/A
化学名 benzyl N-[(2S)-3-methyl-1-oxo-1-[(1-oxo-3-phenylpropan-2-yl)amino]butan-2-yl]carbamate
分子式 C22H26N2O4
分子量 382.45
溶解度 ≥ 16.75mg/mL in DMSO, ≥ 25.05 mg/mL in EtOH with ultrasonic
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
MDL 28170 is a selective inhibitor, which inhibites calpain with Ki values of 10nM and cathepsin B with Ki values of 25 nM while does not inhibit trypsin-like serine proteases. And it can penetrate the blood–brain barrier rapidly and show the activity in inhibiting brain cysteine protease activity following systemic administration [1,2].
Calpain could affect reperfusion function directly through limited proteolysis of the sarcomeres.And function improvement of MDL-28170 during reperfusion were supported byexperimets. It is thought to act by blocking the sites of catalysis ofcalpains. The experiments also showed skinned muscle fibers which was isolated from the tropical of stunned ferret hearts reveal decreased sensitivity to Ca2+, and the decrease in sensitivity could be reversed if MDL-28170 is treated prior to ischemia and during early reperfusion [1].
When peritoneal mouse macrophages were pre-infected with trypomastigotes for 3 h , MDL28170 was able to reduce the viability of bloodstream trypomastigotes significantly with an IC50/24h value of 20.4 mM. Also, asparasitespre-treated with MDL28170 concentration rose from 6.25 to 50 mM, presenting a clear dose-dependent inhibition profile prior to of macrophage, where the corresponding inhibition from 20% increased to 50%. In addition, macrophages experimentally infected with T. cruzi which were treated with MDL 28170 presented a reduction in the percentage of infection even at the lowest concentrations of 6.25 mM [3].
Upon Ca2+ repletion in the isolated heart of rats, the hearts deteriorated immediately, revealing a marked depression in cardiac function and an enlarged myocardial injury area. This was accompanied by significant increases in lactate dehydrogenase, mitochondrial release of cytochrome c, the apoptotic index and degraded TnI. MDL 28170 significantly inhibited these changes, with the exception of TnI degradation [4].
References:
[1]. Urthaler F, Wolkowicz PE, Digerness SB, et al. MDL-28170, a membrane-permeantcalpain inhibitor, attenuates stunning and PKC epsilon proteolysis in reperfused ferret hearts. Cardiovasc Res, 1997, 35 (1): 60-7.
[2]. Li P, Wendy H, He Q, et al. Postischemic treatment withcalpain inhibitor MDL 28170ameliorates brain damage in a gerbil model of global ischemia, Neuroscience Letters, 1998, 247 :17–20.
[3]. V?′tor EV, Rubem F, Andre′ L, Effects of the calpain inhibitor MDL28170 on the clinically relevant forms of Trypanosomacruzi in vitro. J AntimicrobChemother , 2010, 65: 1395–1398.
关键字： 88191-84-8;C22H26N2O4;MDL 28170;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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