| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| Other Sizes |
Purity: = 99.13%
| Targets |
This compound targets trypsin-like serine proteases and other proteases that cleave after arginine residues. Enzymatic cleavage releases the fluorescent AMC group, allowing quantitative measurement of protease activity.
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|---|---|
| ln Vitro |
In vitro, Ac-Leu-Arg-AMC is used as a substrate to measure trypsin-like protease activity in cell lysates, purified enzyme preparations, or biological fluids. Upon cleavage, AMC is released and detected fluorometrically.
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| ln Vivo |
In vivo, this compound is not used as a therapeutic agent. It is employed in ex vivo assays to measure protease activity in tissue lysates or biological samples.
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| Enzyme Assay |
The substrate is incubated with the protease of interest in assay buffer. The reaction is monitored continuously or at end-point by measuring fluorescence (excitation ~360 nm, emission ~460 nm). The increase in fluorescence is proportional to enzyme activity.
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| Cell Assay |
Not applicable as a treatment; this compound is used as a reagent in cell lysates. Cell lysates are prepared and incubated with the substrate to measure intracellular protease activity.
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| Animal Protocol |
Not applicable; this compound is not administered to animals. It is used to measure protease activity in tissue lysates harvested from animals in disease models.
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| ADME/Pharmacokinetics |
As a peptide substrate, Ac-Leu-Arg-AMC is not a drug and does not have pharmacokinetic properties. It is used as an in vitro reagent.
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| Toxicity/Toxicokinetics |
The compound itself is non-toxic as it is used as an in vitro reagent. It is not intended for human use. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
Ac-Leu-Arg-AMC is a widely used research tool in protease biology. It is not a drug and has no clinical development or regulatory approval status.
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| Molecular Formula |
C24H34N6O5
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|---|---|
| Molecular Weight |
486.563965320587
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| Exact Mass |
486.259
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| CAS # |
929621-79-4
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| PubChem CID |
134611626
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| Appearance |
White to off-white solid powder
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| LogP |
0.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
35
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| Complexity |
851
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CC(=O)OC2C=C(C=CC1=2)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)C)CC(C)C
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| InChi Key |
YAPHUDCEMGABMM-OALUTQOASA-N
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| InChi Code |
InChI=1S/C24H34N6O5/c1-13(2)10-19(28-15(4)31)23(34)30-18(6-5-9-27-24(25)26)22(33)29-16-7-8-17-14(3)11-21(32)35-20(17)12-16/h7-8,11-13,18-19H,5-6,9-10H2,1-4H3,(H,28,31)(H,29,33)(H,30,34)(H4,25,26,27)/t18-,19-/m0/s1
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| Chemical Name |
(2S)-2-acetamido-N-[(2S)-5-(diaminomethylideneamino)-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxopentan-2-yl]-4-methylpentanamide
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~300 mg/mL (~616.57 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 | 2.0552 mL | 10.2762 mL | 20.5524 mL | |
| 5 mM | 0.4110 mL | 2.0552 mL | 4.1105 mL | |
| 10 mM | 0.2055 mL | 1.0276 mL | 2.0552 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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