| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 25mg | |||
| Other Sizes |
| Targets |
The primary targets of ALLM are calpain I, calpain II, cathepsin B, and cathepsin L. Calpains are calcium-dependent cysteine proteases involved in various cellular processes, including cell migration, apoptosis, and signal transduction. Cathepsins are lysosomal proteases involved in protein degradation and antigen presentation. By inhibiting these proteases, ALLM can modulate their activities and study their roles in cellular function.
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| ln Vitro |
In vitro, ALLM is a potent inhibitor of calpain I (Ki = 120 nM), calpain II (Ki = 230 nM), cathepsin B (Ki = 100 nM), and cathepsin L (Ki = 600 pM). Its activity is characterized in enzyme assays measuring the cleavage of specific substrates. The compound's cell-permeability allows it to be used in cell-based studies.
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| ln Vivo |
Five days after SCI, ALLM (calpain inhibitor II) (0.5 mg/kg), injected every 24 hours, suppresses calpain activation but not caspase 3. This neuronal cell death is stopped by ALLM [2]. Following spinal cord injury (SCI), ALLM (0.05–2.5 mg/kg; intraperitoneally; every 24 hours for 1 week) lessens movement abnormalities [2].
In vivo, ALLM has been used to demonstrate the involvement of ubiquitin-proteasome pathways in various biological processes. As a cell-permeable inhibitor, it can be administered to animal models to study the roles of calpains and cathepsins in physiology and disease. Its effects are dose-dependent and related to its ability to inhibit these proteases. |
| Enzyme Assay |
In vitro enzyme assays for ALLM measure its inhibition of calpain and cathepsin activity. The enzymes are incubated with a fluorogenic or chromogenic substrate, and the cleavage of the substrate is measured. The compound's Ki values are determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for ALLM evaluate its effects on calpain- and cathepsin-mediated cellular processes. Cells are treated with the compound, and the inhibition of substrate cleavage is measured. The compound's effects on cell migration, apoptosis, or other calpain/cathepsin-dependent processes are assessed.
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| Animal Protocol |
Animal/Disease Models: Adult male Wistar rat (280-300g) (spinal cord injury model) [2]
Doses: 0.05, 0.5 and 2.5 mg/kg Route of Administration: intraperitoneal (ip) injection; every 24 hrs (hrs (hours)) for 1 week Experimental Results: Shown Dramatically better motor function. In vivo animal studies for ALLM are conducted to study the roles of calpains and cathepsins in various disease models. The compound is administered via intraperitoneal or intravenous routes. Its effects on disease progression, such as neurodegeneration or muscle wasting, are assessed. Pharmacodynamic studies measure calpain/cathepsin activity in target tissues. Pharmacokinetic studies determine the compound's half-life and bioavailability. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of ALLM have been characterized in preclinical studies. Its molecular weight is 401.56 g/mol. The compound is soluble in DMSO and should be stored at -20°C. Its solubility in water is approximately 0.52 g/L. Further details on its half-life, Cmax, and bioavailability are available from the primary research literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of ALLM has not been extensively detailed in the available literature. It is classified for research use only and not for human consumption. As a protease inhibitor, its potential side effects may include off-target effects on other proteases. Standard safety precautions for handling bioactive compounds should be followed.
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| References |
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| Additional Infomation |
N-acetylleucyl-leucyl-methionine aldehyde is a peptide.
Additional information: ALLM is also known as Ac-Leu-Leu-Met-H and Calpain Inhibitor II. It is a cell-permeable peptide aldehyde inhibitor of calpain I, calpain II, cathepsin B, and cathepsin L. It is used as a research tool to study the roles of these proteases in various cellular processes. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C19H35N3O4S
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|---|---|
| Molecular Weight |
401.56
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| Exact Mass |
401.234
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| CAS # |
110115-07-6
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| PubChem CID |
121855
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
676.5±55.0 °C at 760 mmHg
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| Flash Point |
362.9±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.496
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| LogP |
2.64
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
27
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| Complexity |
497
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C=O)NC(=O)C
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| InChi Key |
RJWLAIMXRBDUMH-ULQDDVLXSA-N
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| InChi Code |
InChI=1S/C19H35N3O4S/c1-12(2)9-16(20-14(5)24)19(26)22-17(10-13(3)4)18(25)21-15(11-23)7-8-27-6/h11-13,15-17H,7-10H2,1-6H3,(H,20,24)(H,21,25)(H,22,26)/t15-,16-,17-/m0/s1
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| Chemical Name |
(2S)-2-Acetamido-4-methyl-N-[(2S)-4-methyl-1-[[(2S)-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]pentanamide
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| Synonyms |
ALLM Calpain Inhibitor II N-Allm NAllmN Allm
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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) |
Ethanol :≥ 20 mg/mL (~49.81 mM)
DMF :≥ 20 mg/mL (~49.81 mM) DMSO : ≥ 20 mg/mL (~49.81 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4903 mL | 12.4514 mL | 24.9029 mL | |
| 5 mM | 0.4981 mL | 2.4903 mL | 4.9806 mL | |
| 10 mM | 0.2490 mL | 1.2451 mL | 2.4903 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04404504 | Completed | Acute Stroke | University Hospital, Essen | March 20, 2019 |
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