| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
EDANS does not target a specific protein or enzyme itself; rather, it serves as a fluorogenic substrate for retroviral proteases. The compound is designed to be incorporated into peptide substrates that are specifically recognized and cleaved by target proteases. Upon enzymatic cleavage, the fluorescence of EDANS is dequenched, allowing for the detection and quantification of protease activity. The compound's utility is based on its role as a fluorescence donor in resonance energy transfer (RET) assays, where it is paired with a suitable quencher molecule.
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|---|---|
| ln Vitro |
The natural processing site of HIV-1 PR is the source of the peptide sequence of EDANS[1]. When fluorescent substrates are added to recombinant HIV-1 PR, the Tyr-Pro bond is specifically broken and the intensity of the fluorescence increases with time in a manner that is directly proportional to the degree of substrate hydrolysis [1].
The in vitro activity of EDANS is characterized by its function as a fluorogenic substrate in protease activity assays. The compound itself is non-fluorescent or weakly fluorescent when part of an intact FRET peptide substrate due to quenching by an adjacent acceptor molecule. Upon cleavage by a target protease, the EDANS fluorophore is separated from the quencher, resulting in a significant increase in fluorescence intensity. This fluorescence turn-on response enables the sensitive and real-time monitoring of protease activity. EDANS exhibits favorable fluorescence properties, with excitation and emission maxima in the UV-visible range, making it compatible with standard fluorescence detection systems. The compound is commonly used in high-throughput screening (HTS) assays to identify protease inhibitors. |
| ln Vivo |
No significant in vivo activity has been reported for EDANS, as the compound is primarily utilized as an in vitro research tool for biochemical assays rather than as a therapeutic or diagnostic agent. Its application is limited to cell-free and cell-based in vitro systems for studying protease function and screening potential inhibitors.
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| Enzyme Assay |
In vitro enzyme assays using EDANS typically involve the preparation of a fluorogenic peptide substrate containing EDANS as the donor fluorophore and a suitable quencher (such as DABCYL). The substrate is incubated with the target protease in an appropriate buffer at physiological pH. Upon enzymatic cleavage, the fluorescence intensity is measured using a fluorescence microplate reader or fluorometer with excitation and emission wavelengths optimized for EDANS. The increase in fluorescence over time is proportional to protease activity. Inhibitors can be evaluated by measuring the reduction in fluorescence increase in the presence of test compounds.
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| Cell Assay |
For in vitro cellular experiments, EDANS-based substrates are not typically used directly in live-cell assays due to limited cell permeability. However, cell lysates or purified enzyme preparations from treated cells can be incubated with EDANS substrates to assess intracellular protease activity. Alternatively, cell-permeable versions of EDANS substrates may be employed in some specialized applications. Fluorescence detection is performed using flow cytometry or fluorescence microscopy to measure the dequenched signal.
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| Animal Protocol |
In vivo animal experiments with EDANS are not commonly performed, as the compound is primarily utilized as an in vitro research tool. The compound is not intended for systemic administration or therapeutic use. Studies involving EDANS are typically confined to biochemical and cell-based assays.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of EDANS have not been characterized, as the compound is a research-use fluorogenic substrate rather than a drug candidate. The compound is soluble in DMSO and aqueous buffers at appropriate concentrations. Standard storage recommendations include protection from light and storage at -20°C to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicological data for EDANS has not been systematically evaluated, as the compound is intended for research applications only and not for therapeutic use. Standard laboratory safety precautions should be observed when handling this chemical reagent, including the use of appropriate personal protective equipment and working in a well-ventilated area.
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| References | |
| Additional Infomation |
The structure given in the first document
EDANS is a widely used fluorogenic substrate in protease research, particularly for studying retroviral proteases through resonance energy transfer. The compound is available in various purity grades for research applications and serves as a reference standard for analytical purposes. EDANS is a key component in FRET-based protease assays and has contributed significantly to the discovery and development of protease inhibitors. The compound has no clinical or therapeutic applications and has not received regulatory approval for any medical indication. |
| Molecular Formula |
C12H14N2O3S
|
|---|---|
| Molecular Weight |
266.32
|
| Exact Mass |
266.073
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| CAS # |
50402-56-7
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| Related CAS # |
EDANS sodium;100900-07-0
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| PubChem CID |
92329
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| Appearance |
White to off-white solid powder
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| Density |
1.432 g/cm3
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| Melting Point |
>350°C
|
| Index of Refraction |
1.691
|
| LogP |
3.311
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
18
|
| Complexity |
366
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC2=C(C=CC=C2S(=O)(=O)O)C(=C1)NCCN
|
| InChi Key |
SJQRQOKXQKVJGJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H14N2O3S/c13-7-8-14-11-5-1-4-10-9(11)3-2-6-12(10)18(15,16)17/h1-6,14H,7-8,13H2,(H,15,16,17)
|
| Chemical Name |
5-(2-aminoethylamino)naphthalene-1-sulfonic acid
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
DMSO: 13.89 mg/mL (52.16 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.39 mg/mL (5.22 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 13.9 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: ≥ 1.39 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 13.9 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. View More
Solubility in Formulation 3: ≥ 1.39 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7549 mL | 18.7744 mL | 37.5488 mL | |
| 5 mM | 0.7510 mL | 3.7549 mL | 7.5098 mL | |
| 10 mM | 0.3755 mL | 1.8774 mL | 3.7549 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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