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MDL-28170 (Calpain Inhibitor III) is a novel potent, selective, and membrane-permeable cysteine protease inhibitor of calpain that, when administered systemically, quickly crosses the blood-brain barrier. Also inhibiting γ-secretase is MDL-28170.
| Targets |
calpain; Secretase
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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]. |
| 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].
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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.
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| Animal Protocol |
Male Mongolian gerbils
50 mg/kg IP |
| References |
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| Molecular Formula |
C22H26N2O4
|
|---|---|
| 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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| Appearance |
Solid powder
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| SMILES |
CC(C)[C@@H](C(=O)NC(CC1=CC=CC=C1)C=O)NC(=O)OCC2=CC=CC=C2
|
| InChi Key |
NGBKFLTYGSREKK-ANYOKISRSA-N
|
| 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
|
| 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) |
|---|---|
| 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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