| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Matrix metalloproteinases (MMPs), particularly MMP-2 and MMP-9, as well as other metalloproteinases that cleave the PLGL(Dpa)AR peptide sequence between glycine and leucine residues.
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|---|---|
| ln Vitro |
MOCAc-PLGL(Dpa)AR is cleaved by active MMP-2 and MMP-9, releasing the quenched MOCAc fluorophore and producing fluorescence at excitation/emission maxima of 328/420 nm (or 325/400 nm). Activity is quantified by fluorescence increase over time.
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| ln Vivo |
Not applicable; this is a diagnostic substrate, not a therapeutic agent administered in vivo. It is used in ex vivo assays such as zymography to measure MMP activity in tissue lysates or biological fluids.
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| Enzyme Assay |
Peptide (10 microM) is incubated with recombinant MMP-2 or MMP-9 (0.5-5 nM) in assay buffer (50 mM Tris, 150 mM NaCl, 5 mM CaCl2, 0.05% Brij-35, pH 7.5) at 37degC. Fluorescence (λex=328 nm, λem=420 nm) is monitored for 30-60 minutes using a plate reader.
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| Cell Assay |
Not applicable; no cell-based assays are typically performed with this substrate. It is used in biochemical assays with purified enzymes or in conditioned media containing secreted proteases.
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| Animal Protocol |
Not applicable; this substrate is not administered in vivo. Animals may be treated with compounds of interest, and plasma or tissue lysates are collected for ex vivo MMP activity measurement using this substrate.
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| ADME/Pharmacokinetics |
Not applicable as a therapeutic; the substrate is stable in solution and is rapidly degraded by active MMPs with a Km value typically in the low micromolar range (e.g., 2-10 microM for MMP-2/9).
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| Toxicity/Toxicokinetics |
No toxicity; the peptide substrate is non-toxic at concentrations up to 100 microM in biochemical assays. It is used exclusively for research purposes.
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| References | |
| Additional Infomation |
MOCAc-PLGL(Dpa)AR is for research use only, not FDA-approved. It is commonly employed in high-throughput screening for MMP inhibitors and in diagnostics for cancer, arthritis, and cardiovascular diseases.
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| Molecular Formula |
C49H68N14O15
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|---|---|
| Molecular Weight |
1093.14902
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| Exact Mass |
1092.5
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| CAS # |
140430-53-1
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.173
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~91.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.29 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 (2.29 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9148 mL | 4.5739 mL | 9.1479 mL | |
| 5 mM | 0.1830 mL | 0.9148 mL | 1.8296 mL | |
| 10 mM | 0.0915 mL | 0.4574 mL | 0.9148 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.