| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MeOSuc-AAPV-AMC targets human leukocyte elastase and porcine pancreatic elastase, which are serine proteases that cleave elastin and other proteins. Human leukocyte elastase is involved in inflammatory responses and tissue remodeling. The compound is a substrate for these enzymes, not an inhibitor. Upon cleavage by elastase, the AMC (7-amino-4-methylcoumarin) moiety is released, generating a fluorescent signal that can be quantified. This allows for real-time monitoring of elastase activity.
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| ln Vitro |
Advice (This is our suggested protocol, which should be adjusted to suit your particular requirements as it simply offers guidance) [1]. 2. To create the 2× substrate buffer (400 μM), dilute the stock solution about 100 times in reaction buffer. 3. For 40 minutes, soap the enzyme after that. 4. In a 96-well transparent plate, quickly combine 50 μL of substrate buffer and 50 μL of enzyme solution to measure the enzyme activity. 5. Using the FLEXStation fluorescent microplate reader, note any variations in fluorescence.
In vitro, MeOSuc-AAPV-AMC is used as a substrate in enzyme kinetic assays to measure elastase activity. It has a Km of 362 µM for human leukocyte and porcine pancreatic elastase. The compound is hydrolyzed by these elastases but not by cathepsin G, demonstrating substrate specificity. The released AMC fluorescence (Ex=380 nm, Em=460 nm) is proportional to enzyme activity. It is widely used for screening elastase inhibitors in drug discovery programs. |
| ln Vivo |
In vivo, MeOSuc-AAPV-AMC is not typically used as a therapeutic agent but rather as a research tool. It has been used in animal models to study elastase activity and to evaluate the efficacy of elastase inhibitors. The compound can be administered to measure elastase activity in biological fluids or tissues. However, it is primarily used in vitro for biochemical assays rather than in vivo applications. Its use in vivo would be limited by its rapid clearance and potential for non-specific cleavage.
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| Enzyme Assay |
For enzyme kinetic assays, human leukocyte elastase or porcine pancreatic elastase is incubated with MeOSuc-AAPV-AMC at various concentrations (typically 0-1000 µM) in assay buffer (such as 0.1 M HEPES, pH 7.5, 0.5 M NaCl, 0.01% Triton X-100) at 25-37°C. Fluorescence is measured continuously at excitation 380 nm and emission 460 nm using a fluorescence plate reader. Initial reaction rates (V0) are calculated from the linear portion of the fluorescence increase over time. Km and Vmax values are determined by fitting Michaelis-Menten kinetics.
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| Cell Assay |
For inhibitor screening assays, elastase is pre-incubated with test inhibitors at various concentrations for 10-30 minutes, then MeOSuc-AAPV-AMC substrate is added at a concentration near the Km (typically 100-500 µM). Fluorescence is measured continuously, and initial reaction rates are determined. IC50 values for inhibitors are calculated by fitting dose-response curves of percent inhibition versus inhibitor concentration. The assay can be performed in 96-well or 384-well plate formats for high-throughput screening.
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| Animal Protocol |
For in vivo studies, MeOSuc-AAPV-AMC can be used to measure elastase activity in bronchoalveolar lavage fluid (BALF) or plasma samples from animal models of inflammation. Samples are incubated with the substrate, and fluorescence is measured to quantify elastase activity. This can be used to assess the efficacy of elastase inhibitors in vivo. However, the compound itself is not typically administered to animals as a therapeutic agent; it is used as an ex vivo assay reagent.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MeOSuc-AAPV-AMC are not relevant for its use as a research substrate, as it is not intended for therapeutic use. The compound is stable as a solid and is typically dissolved in DMSO or assay buffer for use. Storage is recommended at -20°C for long-term stability. The compound is for research use only and is not for human or veterinary use.
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| Toxicity/Toxicokinetics |
Toxicological data for MeOSuc-AAPV-AMC have not been reported, as it is a research substrate rather than a therapeutic agent. Standard laboratory safety precautions should be followed when handling this compound. It is not intended for human use and is available for research purposes only.
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| References | |
| Additional Infomation |
MeOSuc-AAPV-AMC is a fluorogenic substrate for human leukocyte elastase and porcine pancreatic elastase with a Km of 362 µM. It is hydrolyzed by these elastases but not by cathepsin G. The compound generates blue AMC fluorescence (Ex=380 nm, Em=460 nm) upon cleavage. It is used in research for studying enzyme kinetics and screening for protease inhibitors in drug development. MeOSuc-AAPV-AMC is a research tool and is not approved for clinical use.
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| Molecular Formula |
C31H41N5O9
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|---|---|
| Molecular Weight |
627.68500
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| Exact Mass |
627.29
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| CAS # |
72252-90-5
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| PubChem CID |
25108618
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
983.7±65.0 °C at 760 mmHg
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| Flash Point |
548.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.570
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| LogP |
1.99
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
45
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=CC(=O)OC2=C1C=CC(=C2)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]3CCCN3C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)CCC(=O)OC
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| InChi Key |
CMEUDEVBFFPSEI-NFHWZJRKSA-N
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| InChi Code |
InChI=1S/C31H41N5O9/c1-16(2)27(30(42)34-20-9-10-21-17(3)14-26(39)45-23(21)15-20)35-29(41)22-8-7-13-36(22)31(43)19(5)33-28(40)18(4)32-24(37)11-12-25(38)44-6/h9-10,14-16,18-19,22,27H,7-8,11-13H2,1-6H3,(H,32,37)(H,33,40)(H,34,42)(H,35,41)/t18-,19-,22-,27-/m0/s1
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| Chemical Name |
methyl 4-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-3-methyl-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-oxobutanoate
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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 : ~125 mg/mL (~199.14 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 | 1.5931 mL | 7.9657 mL | 15.9314 mL | |
| 5 mM | 0.3186 mL | 1.5931 mL | 3.1863 mL | |
| 10 mM | 0.1593 mL | 0.7966 mL | 1.5931 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.
Products are for research use only; We do not sell to patients
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