| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Caspase-1 AChE
Mca-YVADAP-Lys(Dnp)-OH TFA targets the active sites of caspase-1 (a cysteine protease involved in inflammatory cytokine processing) and ACE2 (a carboxypeptidase important in the renin-angiotensin system). The YVAD sequence is the recognition motif for caspase-1. |
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| ln Vitro |
The peptide is specifically cleaved by caspase-1 and ACE2 at the designated scissile bonds. Upon enzymatic cleavage, the Mca fluorophore is spatially separated from the Dnp quencher, resulting in a dramatic increase in fluorescence emission, typically 10- to 100-fold above baseline.
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| ln Vivo |
Not available. Mca-YVADAP-Lys(Dnp)-OH TFA is not a therapeutic agent and does not exhibit intrinsic pharmacological activity in vivo. It is strictly a research tool for ex vivo or in vitro enzymatic activity measurements in tissue lysates or biological fluids.
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| Enzyme Assay |
Standard enzyme kinetic assays involve incubating the substrate (1-50 uM) with recombinant caspase-1 (1-10 nM) or ACE2 (5-50 ng/uL) in assay buffer (e.g., 50 mM HEPES, pH 7.4, containing 100 mM NaCl, 0.1% CHAPS, 10 mM DTT for caspase-1) at 37degC for 30-120 minutes in a black 96-well plate. Fluorescence is monitored continuously (excitation 320-340 nm, emission 390-420 nm) or at endpoint intervals. Kinetic parameters Km and Vmax are calculated by fitting fluorescence intensity vs time data.
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| Cell Assay |
Not available. For cellular assays, typical protocols involve lysing cells of interest (e.g., THP-1 macrophages treated with LPS and ATP) in lysis buffer, clarifying lysates by centrifugation, incubating 50-100 uL lysate with 10-50 uM substrate in assay buffer at 37degC for 1-2 hours, and measuring fluorescence increase to quantify caspase-1 or ACE2 activity.
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| Animal Protocol |
Not available. For ex vivo tissue assays, standard protocols involve homogenizing tissues (e.g., brain, kidney, heart) in cold lysis buffer, centrifuging to remove debris, incubating 100-200 ug protein homogenate with 10-50 uM substrate at 37degC for 1-4 hours, and measuring fluorescence to assess disease-related enzyme activity changes.
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| ADME/Pharmacokinetics |
Not available. The TFA salt form enhances substrate solubility and stability. As a synthetic peptide, it is stable for months when stored desiccated at -20degC. In solution, stability is limited; working solutions should be prepared fresh and used within hours.
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| Toxicity/Toxicokinetics |
Not available. The compound is generally non-toxic at typical assay concentrations (1-100 uM). As a peptide, it poses minimal safety risks in laboratory settings. No specific toxicological studies have been reported, as it is not intended for in vivo administration.
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| References | |
| Additional Infomation |
Mca-YVADAP-Lys(Dnp)-OH TFA is a research-grade FRET substrate widely used to study inflammasome activation, inflammatory diseases (e.g., sepsis, arthritis), and ACE2 biology relevant to cardiovascular and coronavirus research. The TFA counterion improves aqueous solubility. This product has not been evaluated in clinical trials.
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| Molecular Formula |
C55H65F3N10O21
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|---|---|
| Molecular Weight |
1259.15
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| Related CAS # |
Mca-YVADAP-Lys(Dnp)-OH;189696-01-3
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| Appearance |
White to yellow solid powder
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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) |
H2O :~22.22 mg/mL (~17.65 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7942 mL | 3.9709 mL | 7.9419 mL | |
| 5 mM | 0.1588 mL | 0.7942 mL | 1.5884 mL | |
| 10 mM | 0.0794 mL | 0.3971 mL | 0.7942 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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