| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
MMP-1 27.5 μM (Km) MMP-8 MMP-13 5.2 μM (Km) MMP-14 7.9 μM (Km)
A wide range of matrix metalloproteinases (MMPs), including MMP-1, -2, -7, -8, -9, -13, and -17. This peptide serves as an improved FRET substrate for these enzymes, with enhanced substrate properties compared to the standard Mca-PLGL-Dpa-AR-NH2 substrate. |
|---|---|
| ln Vitro |
Specificity for collagenase (MMP-1, MMP-8, MMP-13) and MT1-MMP (MMP-14): Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH26 The constant (kcat/Km) is increased by 2–9 times, or 3 times, in comparison with FS-1 [1].
This compound is a highly sensitive FRET substrate for MMPs. It is cleaved by multiple MMP isoforms, including gelatinases (MMP-2, -9), collagenases (MMP-1, -8, -13), and matrilysin (MMP-7). The N-terminal elongation with a Lys residue improves its specificity constant (kcat/Km) and overall substrate properties, making it a superior tool for measuring MMP activity. |
| ln Vivo |
As a research substrate, Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 has no in vivo activity of its own. However, it is widely used for ex vivo analyses. It can be used to measure MMP activity in tissue lysates or biological fluids from animal models of cancer, arthritis, fibrosis, and other diseases where MMPs are dysregulated.
|
| Enzyme Assay |
For non-cellular assays, the FRET substrate is diluted to the desired concentration (e.g., 5-20 uM) in an assay buffer (e.g., 50 mM Tris-HCl, pH 7.5, 10 mM CaCl2, 150 mM NaCl). The reaction is initiated by adding the MMP enzyme (1-10 nM). The increase in fluorescence is measured (excitation 325 nm, emission 393 nm) using a fluorescence plate reader. The initial reaction velocity (V0) is calculated from the linear portion of the curve.
|
| Cell Assay |
Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 is not a drug, so it is not used in standard cell-based assays for toxicity or efficacy. Instead, cells are treated with test compounds (e.g., MMP inhibitors or activators). Then, the cells are lysed, and the cleared lysate is incubated with this FRET substrate to measure MMP activity. The fluorescence signal is normalized to total protein concentration determined by a BCA assay.
|
| Animal Protocol |
For ex vivo activity measurements, animals are treated with test compounds or disease models are induced. Tissues (e.g., tumor, synovium) or bodily fluids (e.g., plasma, synovial fluid) are collected and homogenized. The lysate is clarified by centrifugation. The protein concentration is quantified, and the cleared lysate is incubated with the FRET substrate. The resulting increase in fluorescence is measured to calculate MMP activity.
|
| ADME/Pharmacokinetics |
The compound itself is a peptide with a molecular weight of 1221.34 g/mol and is stored as a solid at -20degC, protected from light. The peptide is soluble in water and is typically reconstituted in DMSO to make a stable stock solution (e.g., 10 mM). Once in solution, it is stable for several hours, but long-term storage should be as a dry powder at -20degC.
|
| Toxicity/Toxicokinetics |
The Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 peptide is not toxic at the concentrations used in standard activity assays (1-50 uM). However, standard laboratory safety precautions for handling research chemicals should be followed. Appropriate personal protective equipment (PPE), such as gloves and a lab coat, should be worn at all times.
|
| References | |
| Additional Infomation |
This FRET substrate is a widely used research tool for studying MMP activity in drug discovery. It is also known by the synonym FS-6. It is often used in high-throughput screening (HTS) to discover new MMP inhibitors. It is an improved version of the classic MMP FRET substrate Mca-PLGL-Dpa-AR-NH2. Its structure and mechanism of action (FRET) make it a valuable tool for studying MMP biology.
|
| Molecular Formula |
C55H80N16O16
|
|---|---|
| Molecular Weight |
1221.32
|
| Exact Mass |
1220.59
|
| CAS # |
720710-69-0
|
| PubChem CID |
91869387
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
5.663
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
33
|
| Heavy Atom Count |
87
|
| Complexity |
2500
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N)NC(=O)[C@H](CNC1=C(C=C(C=C1)[N+](=O)[O-])[N+](=O)[O-])NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)CC3=CC(=O)OC4=C3C=CC(=C4)OC
|
| InChi Key |
KODVNTQEXXMHSL-XKDADYKASA-N
|
| InChi Code |
InChI=1S/C55H80N16O16/c1-29(2)21-39(67-53(80)42-13-10-20-69(42)54(81)38(11-7-8-18-56)64-45(72)23-32-24-47(74)87-44-26-34(86-6)15-16-35(32)44)50(77)62-28-46(73)65-40(22-30(3)4)51(78)68-41(27-61-36-17-14-33(70(82)83)25-43(36)71(84)85)52(79)63-31(5)49(76)66-37(48(57)75)12-9-19-60-55(58)59/h14-17,24-26,29-31,37-42,61H,7-13,18-23,27-28,56H2,1-6H3,(H2,57,75)(H,62,77)(H,63,79)(H,64,72)(H,65,73)(H,66,76)(H,67,80)(H,68,78)(H4,58,59,60)/t31-,37-,38-,39-,40-,41-,42-/m0/s1
|
| Chemical Name |
(2S)-N-[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(2,4-dinitroanilino)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]-1-[(2S)-6-amino-2-[[2-(7-methoxy-2-oxochromen-4-yl)acetyl]amino]hexanoyl]pyrrolidine-2-carboxamide
|
| 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, avoid exposure to moisture. |
| 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) |
DMSO: 100 mg/mL (81.88 mM)
H2O: 10 mg/mL (8.19 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8188 mL | 4.0939 mL | 8.1879 mL | |
| 5 mM | 0.1638 mL | 0.8188 mL | 1.6376 mL | |
| 10 mM | 0.0819 mL | 0.4094 mL | 0.8188 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
