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| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide targets the active site of TACE (ADAM-17, a disintegrin and metalloproteinase 17), the enzyme responsible for cleaving membrane-bound pro-TNF-alpha to release soluble, bioactive TNF-alpha. The peptide sequence spans residues -5 to +6 of the human TNF-alpha cleavage site.
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| ln Vitro |
Enzymatic activity is determined by fluorescence intensity change upon cleavage. The Mca fluorophore and Dnp quencher are positioned such that intact substrate exhibits low fluorescence. Upon TACE-mediated cleavage at the specific peptide bond, Mca and Dnp separate, producing a measurable increase in fluorescence (excitation ~320 nm, emission ~405 nm).
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| ln Vivo |
Not available. This FRET peptide is not a therapeutic agent and does not exhibit intrinsic in vivo activity. It serves exclusively as a research tool to measure TACE activity in vitro or ex vivo, enabling study of sheddase function in inflammation and disease.
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| Enzyme Assay |
Standard TACE kinetic assays involve incubating 5-50 uM substrate with 1-50 nM recombinant human TACE catalytic domain in assay buffer (e.g., 50 mM HEPES, pH 7.4, containing 0.005% Brij-35, 10 uM ZnCl2) at 37degC for 30-120 minutes. Fluorescence is monitored continuously (excitation 320-340 nm, emission 400-420 nm) using a microplate reader. Kinetic parameters are derived by fitting progress curves.
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| Cell Assay |
Not available. For cellular TACE activity measurement, typical protocols involve lysing cells (e.g., LPS-stimulated macrophages) in Triton X-100-containing buffer, centrifuging, incubating 50-200 ug lysate protein with 10-50 uM substrate in assay buffer at 37degC for 2-4 hours, and measuring fluorescence increase relative to controls containing TACE inhibitor (e.g., TAPI-1).
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| Animal Protocol |
Not available. For ex vivo tissue studies, standard protocols involve homogenizing tissues (e.g., mouse heart, lung, or brain) in lysis buffer, centrifuging to obtain clarified lysates, incubating 100-200 ug protein homogenate with 10-50 uM substrate at 37degC for 2-6 hours, and measuring fluorescence to assess disease-related TACE activity changes in models of inflammation, arthritis, or cancer.
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| ADME/Pharmacokinetics |
Not available. The TFA salt improves solubility in aqueous buffers. As a synthetic peptide, it is stable for months when stored at -20degC. In solution, the substrate is susceptible to spontaneous hydrolysis; working solutions should be prepared fresh and protected from light.
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| Toxicity/Toxicokinetics |
Not available. This FRET substrate is generally non-toxic at typical assay concentrations (1-100 uM). No toxicological studies have been reported, as the compound is intended exclusively for in vitro laboratory research and not for in vivo administration.
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| References |
[1]. Yi Wang, et al. Protease assay method using site-specific fluorescence dye labeled protein as substrate. US9708638. 2017.
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| Additional Infomation |
Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide is a research-grade FRET substrate used to study ADAM-17/TACE biology in inflammation, cancer, and cardiovascular disease. It has not entered clinical trials. The TFA salt enhances handling. This product is for laboratory use only.
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| Molecular Formula |
C69H103N23O24.C2HF3O2
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| Related CAS # |
Mca-(endo-1a-Dap(Dnp))-TNF-Alpha (-5 to +6) amide (human);192723-42-5
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| Appearance |
Typically exists as solid at room temperature
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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, 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)
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| Solubility (In Vitro) |
H2O :~12.5 mg/mL (~7.13 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.) |
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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