MDL 28170 (Synonyms: MDL 28170) |
Catalog No.GC11640 |
A cell permeable, selective calpain inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 88191-84-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
[4]. Bi S H, Jin Z X, Zhang J Y, et al. Calpaininhibi tor MDL 28170 protectsagainst the Ca2+paradox in rat hearts.Clinical and Experimental Pharmacology and Physiology , 2012, 39:385–392 .
Cas No. | 88191-84-8 | SDF | |
Synonyms | MDL 28170 | ||
Chemical Name | benzyl N-[(2S)-3-methyl-1-oxo-1-[(1-oxo-3-phenylpropan-2-yl)amino]butan-2-yl]carbamate | ||
Canonical SMILES | CC(C)C(C(=O)NC(CC1=CC=CC=C1)C=O)NC(=O)OCC2=CC=CC=C2 | ||
Formula | C22H26N2O4 | M.Wt | 382.45 |
Solubility | ≥ 16.75mg/mL in DMSO, ≥ 25.05 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL |
5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL |
10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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