| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Boc-Leu-Gly-Arg-AMC targets plasmin, a serine protease that plays a key role in fibrinolysis, the process of breaking down blood clots. Plasmin cleaves the peptide bond between the arginine residue and the AMC group, releasing the fluorophore. The Boc protecting group provides stability to the peptide. The compound is also a substrate for other serine proteases with similar substrate specificity, such as trypsin and tissue plasminogen activator (tPA).
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| ln Vitro |
In order to prove that the abdominal glands contain proteolytic enzymes that can produce Sodefrin, an enzymatic test was created with the synthetic substrate Boc-Leu-Gly-Arg-AMC. The hydrolysis of Boc-Leu-Gly-Arg-AMC by crude extracts of the abdominal glands releases 7-amino-4-methylcoumarin, a sign that the gland contains an enzyme that converts sodefrin from its precursor molecule. At pH 9.0 and 45°C, the extract's ability to cleave Boc-Leu-Gly-Arg-AMC is at its peak [1].
In vitro, Boc-Leu-Gly-Arg-AMC is used to measure plasmin activity in a variety of biological samples, including plasma, serum, and tissue homogenates. The compound is incubated with the sample, and the fluorescence of the released AMC is measured over time using a fluorometer. The rate of fluorescence increase is proportional to the plasmin activity in the sample. Boc-Leu-Gly-Arg-AMC is also used in high-throughput screening assays to identify plasmin inhibitors. |
| ln Vivo |
In vivo, Boc-Leu-Gly-Arg-AMC is not typically used as a therapeutic agent; it is primarily a research tool for measuring plasmin activity. However, the measurement of plasmin activity in biological samples has important implications for the diagnosis and monitoring of diseases involving the fibrinolytic system, such as thrombosis and bleeding disorders.
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| Enzyme Assay |
In vitro enzyme assays for Boc-Leu-Gly-Arg-AMC are performed by incubating the compound with plasmin or other serine proteases in a buffer at 37°C. The release of AMC is monitored continuously using a fluorometer with excitation at 360-380 nm and emission at 440-460 nm. The initial rate of fluorescence increase is proportional to the enzyme activity. The assay can be used to determine the kinetic parameters, such as Km and Vmax, of the enzyme for the substrate.
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| Cell Assay |
In vitro cellular experiments for Boc-Leu-Gly-Arg-AMC are not typically performed, as the compound is a substrate for secreted or extracellular proteases rather than intracellular enzymes. However, the compound can be used to measure plasmin activity in cell culture supernatants or in cell-based assays where plasmin is secreted.
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| Animal Protocol |
In vivo animal studies for Boc-Leu-Gly-Arg-AMC are not typically conducted, as the compound is a research tool for measuring enzyme activity rather than a therapeutic agent. However, the compound can be used to measure plasmin activity in plasma or tissue extracts from animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not applicable to Boc-Leu-Gly-Arg-AMC, as it is a research tool rather than a therapeutic agent. The compound is used in vitro as a substrate for enzyme assays.
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| Toxicity/Toxicokinetics |
Toxicology is not applicable to Boc-Leu-Gly-Arg-AMC, as it is a research tool rather than a therapeutic agent. The compound is generally considered safe for handling in the laboratory under standard safety precautions. It is not known to be toxic, mutagenic, or carcinogenic.
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| References |
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| Additional Infomation |
Boc-Leu-Gly-Arg-AMC is a fluorogenic peptide substrate for plasmin and other serine proteases. Upon cleavage by plasmin, the AMC group is released, producing a fluorescent signal that can be quantified. This compound is used in research to measure plasmin activity and to screen for plasmin inhibitors. It is a valuable tool for studying the fibrinolytic system and for the development of therapeutics targeting plasmin.
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| Molecular Formula |
C29H43N7O7
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|---|---|
| Molecular Weight |
601.6944
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| Exact Mass |
601.322
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| CAS # |
65147-09-3
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| PubChem CID |
53765602
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| Appearance |
White to off-white solid powder
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| LogP |
4.28
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
43
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=CC(=O)OC2=C1C=CC(=C2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C
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| InChi Key |
DLAQYOHJZUTWDJ-SFTDATJTSA-N
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| InChi Code |
InChI=1S/C29H43N7O7/c1-16(2)12-21(36-28(41)43-29(4,5)6)25(39)33-15-23(37)35-20(8-7-11-32-27(30)31)26(40)34-18-9-10-19-17(3)13-24(38)42-22(19)14-18/h9-10,13-14,16,20-21H,7-8,11-12,15H2,1-6H3,(H,33,39)(H,34,40)(H,35,37)(H,36,41)(H4,30,31,32)/t20-,21-/m0/s1
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| Chemical Name |
tert-butyl N-[(2S)-1-[[2-[[(2S)-5-(diaminomethylideneamino)-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]carbamate
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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 : ~100 mg/mL (~166.20 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.15 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 25.0 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: ≥ 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6620 mL | 8.3099 mL | 16.6199 mL | |
| 5 mM | 0.3324 mL | 1.6620 mL | 3.3240 mL | |
| 10 mM | 0.1662 mL | 0.8310 mL | 1.6620 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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