| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
calpain; Secretase
MDL-28170 targets calpain-1, calpain-2, and cathepsin B, with Ki values of 10 and 25 nM, respectively. It also inhibits γ-secretase. By inhibiting calpains, it prevents the proteolysis of various substrates involved in cell signaling, apoptosis, and neurodegeneration. This makes it a valuable tool for studying these processes. |
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| ln Vitro |
MDL-28170 enhances the synaptic response recovery in hippocampus slices after extended, moderate hypoxia without causing hypoxic depolarization in a significant and time-dependent manner[1].
MDL-28170 inhibits brain cysteine proteinase activity in a dose-dependent manner (in vitro Ki= 0.01 μM)[2]. In vitro, MDL-28170 demonstrates potent inhibitory activity against its targets. It shows Ki values of 10 nM for calpain and 25 nM for cathepsin B. It has an EC50 value of 14 µM in a cell-based assay. It has also been shown to be an effective antiviral agent, inhibiting SARS-CoV replication in Vero 76 cells with an IC50 of 10 µM. |
| ln Vivo |
Four animals in each of the two treatment groups receive treatment with MDL-28170 (50 mg/kg, i.p.) to totally prevent striatal damage. When MDL-28170 injections are administered to animals at 0.5 and 3 hours of recirculation, respectively, the number of necrotic neurons is decreased by 85% and 68%[2].
MDL-28170 (30 mg/kg, i.p.) decreases the corpus callosum's structural and functional degradation after fluid percussion injury[3].
MDL-28170 (10 mg/kg, i.p.) dramatically enhances nerve function metrics. In diabetic rats, nociceptive behavior is improved by MDL-28170 (3 and 10 mg/kg, i.p.) in diabetic rats[5].
In vivo, MDL-28170 shows neuroprotective effects. It can attenuate depression in myocardial contractile performance that occurs during reperfusion following cardiac ischemia. Its calpain inhibitory activity is responsible for these protective effects. It is used as a research tool to study the role of calpains in various diseases. |
| Enzyme Assay |
The in vitro enzyme assay for MDL-28170 involves measuring its ability to inhibit calpain activity. The enzyme is incubated with a fluorogenic peptide substrate in the presence of varying concentrations of the compound. The rate of substrate cleavage is measured, and the Ki or IC50 is calculated from the inhibition curve. Similar assays are used for cathepsin B and γ-secretase.
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| Cell Assay |
To evaluate MDL28170's capacity to prevent H2O2-mediated necrosis. MDL28170 (50 nM, 500 nM, 5 μM, or 50 μM) is used to treat cells. For the duration of the experiment, a new drug and H2O2 solution is added to the cells after a one-hour drug pretreatment. The number of live or dead cells is counted three hours after exposure.
In vitro cell culture studies for MDL-28170 utilize various cell lines. Its neuroprotective effects can be studied in neuronal cells subjected to excitotoxicity or ischemia. Its antiviral activity can be studied in Vero 76 cells infected with SARS-CoV. Cell viability is assessed using MTT assays. Apoptosis and cell death are measured by flow cytometry. |
| Animal Protocol |
Male Mongolian gerbils
50 mg/kg IP In vivo animal experiments for MDL-28170 have been performed in models of cardiac ischemia-reperfusion injury. In these studies, the compound is administered, and myocardial contractile performance is measured. Its neuroprotective effects could be studied in models of stroke or traumatic brain injury. Its antiviral efficacy could be studied in animal models of SARS-CoV infection. |
| ADME/Pharmacokinetics |
MDL-28170 has a molecular formula of C22H26N2O4 and a molecular weight of 382.45 g/mol. It is a solid compound that is soluble in DMSO (up to 75 mg/mL). It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. It is a cell-permeable compound.
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| Toxicity/Toxicokinetics |
Toxicological data for MDL-28170 are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed. Its calpain inhibitory activity suggests it could have significant biological effects.
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| References |
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| Additional Infomation |
Z-Val-Phe-H is a dipeptide formed by the condensation of the carboxyl group of N-benzyloxycarbonyl-L-valine with the amino group of L-phenylalanine aldehyde. It is a potent inhibitor of cell-permeable calpains I and II, and also a γ-secretase inhibitor. It functions as an inhibitor of EC 3.4.22.53 (calpain-2), EC 3.4.22.52 (calpain-1), EC 3.4.23.46 (membrane protease 2), an anti-leishmaniasis drug, and an inhibitor of apoptosis. It is an aldehyde, a dipeptide, and a carbamate.
MDL-28170 is a research compound with no clinical approval. It is a valuable tool for studying calpain biology and the role of calpains in cell signaling, apoptosis, neurodegeneration, and ischemia-reperfusion injury. It is also used to study the role of γ-secretase in Alzheimer's disease. Its antiviral activity makes it a compound of interest for research into viral infections. |
| Molecular Formula |
C22H26N2O4
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|---|---|
| Molecular Weight |
382.45284
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| Exact Mass |
382.19
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| Elemental Analysis |
C, 69.09; H, 6.85; N, 7.32; O, 16.73
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| CAS # |
88191-84-8
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| Related CAS # |
88191-84-8
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| PubChem CID |
72430
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
450.4±45.0 °C at 760 mmHg
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| Flash Point |
226.2±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.571
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| LogP |
3.77
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
28
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| Complexity |
497
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(C1C=CC=CC=1)C(C=O)NC(=O)[C@H](C(C)C)NC(=O)OCC1C=CC=CC=1
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| InChi Key |
NGBKFLTYGSREKK-ANYOKISRSA-N
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| InChi Code |
InChI=1S/C22H26N2O4/c1-16(2)20(24-22(27)28-15-18-11-7-4-8-12-18)21(26)23-19(14-25)13-17-9-5-3-6-10-17/h3-12,14,16,19-20H,13,15H2,1-2H3,(H,23,26)(H,24,27)/t19?,20-/m0/s1
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| Chemical Name |
benzyl N-[(2S)-3-methyl-1-oxo-1-[(1-oxo-3-phenylpropan-2-yl)amino]butan-2-yl]carbamate
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| Synonyms |
MDL 28170; MDL-28170; MDL28170
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 30~76 mg/mL (78.4~198.7 mM)
Ethanol: ~10 mg/mL (~26.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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