| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA targets matrix metalloproteinases (MMPs), a family of zinc-dependent endopeptidases that are responsible for the degradation of extracellular matrix components. MMPs play critical roles in physiological processes such as embryonic development, tissue remodeling, and wound healing, as well as in pathological conditions including cancer metastasis, arthritis, and cardiovascular diseases. The peptide sequence Pro-Leu-Gly-Leu is a recognition motif for MMP cleavage. When MMPs cleave the peptide between the Gly and Leu residues, the Mca fluorophore is separated from the quencher (Dap or Dap(Dnp)), resulting in a fluorescence increase that can be quantified. The compound is used as a substrate for various MMP family members, allowing researchers to measure enzyme activity and screen for potential MMP inhibitors. The specific MMP isoforms that cleave this substrate may vary, and the substrate can be used for multiple MMP types.
|
|---|---|
| ln Vitro |
In vitro activity of Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA is measured by its cleavage by MMPs, which results in increased fluorescence. The compound itself is a substrate, not an inhibitor or activator, so its "activity" is defined by its susceptibility to MMP-mediated cleavage. The Mca fluorophore exhibits excitation at approximately 325 nm and emission at approximately 393 nm. Upon cleavage by MMPs, the fluorescence increases proportionally to the amount of substrate cleaved, allowing for quantitative measurement of MMP activity. The compound is typically used in in vitro enzyme assays to measure MMP activity in purified enzyme preparations, cell culture supernatants, or tissue extracts. The substrate's sensitivity and specificity make it a valuable tool for studying MMP function and for screening MMP inhibitors. The TFA salt form enhances solubility for assay applications.
|
| ln Vivo |
In vivo activity of Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA is not applicable in the context of therapeutic or pharmacological activity, as the compound is a fluorogenic substrate rather than a drug. Its "in vivo" application is limited to use in research settings, such as measuring MMP activity in biological samples or using it as a probe to study MMP activity in vivo. However, the compound itself is not administered as a therapeutic agent. It can be used to measure MMP activity in tissue homogenates, plasma, or other biological fluids, providing information about MMP activity in various disease states. The compound's fluorescence properties enable sensitive detection of MMP activity, making it a valuable research tool for studying the role of MMPs in physiology and disease. It is not intended for human use.
|
| Enzyme Assay |
In vitro enzyme assay protocols for Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA typically involve incubating the fluorogenic substrate with MMP enzymes and measuring the increase in fluorescence over time. A standard protocol would involve preparing MMP enzyme (e.g., recombinant MMP-1, MMP-2, MMP-9, or other MMPs) in assay buffer (e.g., Tris-HCl, pH 7.5, with NaCl, CaCl2, ZnCl2, and Brij-35) and adding the substrate at a concentration typically ranging from 1 to 10 μM. The reaction is carried out at 37°C for 30-120 minutes, and fluorescence is measured at excitation/emission wavelengths of 325/393 nm using a fluorescence plate reader. The increase in fluorescence is proportional to enzyme activity. For inhibitor screening, the compound is incubated with varying concentrations of the test inhibitor before adding the substrate, and the inhibition of fluorescence increase is measured. Appropriate controls include substrate-only (no enzyme) and enzyme-only (no inhibitor) wells. Km and Vmax values can be determined from Michaelis-Menten kinetics using varying substrate concentrations.
|
| Cell Assay |
In vitro cell-based assay protocols for Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA typically involve measuring MMP activity secreted by cultured cells or present in cell lysates. A standard protocol would involve seeding cells (e.g., cancer cells, fibroblasts, or macrophages) in culture media, allowing them to grow to confluence, and then collecting conditioned media after a defined period (e.g., 24-48 hours). The conditioned media is incubated with the fluorogenic substrate (typically 1-10 μM) in assay buffer at 37°C for 30-120 minutes, and fluorescence is measured at 325/393 nm. The increase in fluorescence reflects MMP activity in the conditioned media. For inhibitor studies, cells can be treated with test compounds before collecting conditioned media, or inhibitors can be added directly to the assay. Cell viability should be assessed to ensure that observed effects are not due to cytotoxicity. The substrate can also be used in zymography or in situ zymography applications.
|
| Animal Protocol |
In vivo animal experimental protocols are not applicable to Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA as a directly administered compound, as it is a fluorogenic substrate rather than a drug. The compound is not used in animal studies in its native form. However, the substrate can be used to measure MMP activity in tissue samples collected from animal models of disease. A typical protocol would involve collecting tissue samples (e.g., tumors, inflamed tissues, or wound tissues) from animals, homogenizing the tissue in assay buffer, centrifuging to remove debris, and incubating the supernatant with the fluorogenic substrate. The increase in fluorescence is measured to quantify MMP activity in the tissue. This approach can be used to assess the role of MMPs in disease progression or to evaluate the efficacy of MMP inhibitors in vivo. However, the substrate itself is not administered to animals.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties are not applicable to Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA, as the compound is a fluorogenic substrate used in biochemical assays rather than a drug. The compound is not intended for in vivo administration, and its PK properties have not been characterized. The compound is soluble in aqueous buffers and organic solvents, enabling its use in a variety of assay formats. The TFA salt form enhances solubility. It should be stored under recommended conditions to maintain stability. The compound is intended for research use only and is not intended for human use.
|
| Toxicity/Toxicokinetics |
Toxicological data for Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA are limited, as the compound is intended for research use only and has not undergone systematic toxicity testing. No acute toxicity (LD50), subchronic toxicity, genotoxicity, or reproductive toxicity studies have been reported specifically for this compound. As with all research chemicals, appropriate safety precautions should be taken when handling the compound, including working in a fume hood, wearing appropriate personal protective equipment, and avoiding inhalation, ingestion, or skin contact. The compound is not intended for human use. Researchers should consult the material safety data sheet (MSDS) for specific safety information and handling recommendations.
|
| References | |
| Additional Infomation |
Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 TFA is a research-grade fluorogenic peptide substrate used for measuring matrix metalloproteinase (MMP) activity. It contains a Mca fluorophore (excitation 325 nm, emission 393 nm) and a quencher group. Upon cleavage by MMPs, the fluorescence increases, allowing for sensitive and quantitative measurement of enzyme activity. The compound is used in biochemical and cell-based assays to study MMP function, screen MMP inhibitors, and investigate the role of MMPs in diseases such as cancer, inflammation, and tissue remodeling. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action is as a substrate for MMPs, enabling the measurement of enzyme activity. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications.
|
| Molecular Formula |
C43H66N12O11.XC2HF3O2
|
|---|---|
| Molecular Weight |
927.06 (free base)
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
|
|---|---|
| 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.) |
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
Copyright 2020 InvivoChem LLC | All Rights Reserved
