| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Thioredoxin reductase (TrxR) is the primary molecular target. The probe is designed to selectively detect TrxR activity, which plays a key role in maintaining cellular redox homeostasis.
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| ln Vitro |
Fast-TRFS achieves its peak fluorescence signal after 1 minute of TCEP incubation and 5 minutes of TrxR enzyme incubation[1]. In HeLa cells, Fast-TRFS (10 μM; 2-60 min) causes the blue fluorescence signal to develop in less than two minutes[1].
Fast-TRFS is a selective and superfast fluorogenic probe of thioredoxin reductase (TrxR). It exhibits a rapid fluorescence turn-on response upon interaction with TrxR in cell-free assays. The reaction is specific for TrxR and does not cross-react with other reductases. |
| ln Vivo |
There is no specific in vivo activity data available for this compound. However, as a fluorescent probe for enzyme activity, similar compounds are typically used for real-time imaging of TrxR activity in live cells and animal models.
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| Enzyme Assay |
A standard protocol involves incubating Fast-TRFS (e.g., 5 uM) with purified TrxR enzyme and its substrate (NADPH) in a buffer solution (e.g., PBS, pH 7.4) at room temperature. The increase in fluorescence intensity over time is measured using a fluorescence spectrophotometer.
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| Cell Assay |
A general protocol involves seeding cells in a confocal dish and incubating with Fast-TRFS (e.g., 1-10 uM) for 20-30 minutes at 37degC. After washing, live-cell imaging is performed using a confocal microscope to monitor TrxR activity in real-time. A TrxR inhibitor (e.g., auranofin) can be used as a control.
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| Animal Protocol |
A typical protocol for in vivo imaging involves intravenous or intraperitoneal injection of an optimized concentration of Fast-TRFS into a live animal model. After a suitable circulation time (e.g., 30 minutes to 2 hours), the animal is placed under an in vivo imaging system to monitor TrxR activity-induced fluorescence.
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| ADME/Pharmacokinetics |
General PK properties for small molecule probes are not applicable, as these compounds are typically used for acute imaging. However, formulation can be in PBS or saline with co-solvents like DMSO for in vivo use.
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| Toxicity/Toxicokinetics |
General toxicity for imaging probes is considered low. For Fast-TRFS, no specific toxicity studies are reported. In similar experiments, incubation with up to 10 uM for 24 hours in cell models shows good biocompatibility and no significant cytotoxicity.
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| References | |
| Additional Infomation |
Fast-TRFS is a research tool for studying cellular redox biology, particularly the role of the thioredoxin system in cancer, oxidative stress, and drug resistance. Its superfast response allows for real-time monitoring of TrxR activity.
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| Exact Mass |
376.016
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|---|---|
| CAS # |
2966536-18-3
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| PubChem CID |
146168837
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
550
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(CSS1)NC(=O)NC2=CC3=C(C=C2)C(=CC(=O)O3)C(F)(F)F
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| InChi Key |
WRYRCLGYENFDIB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11F3N2O3S2/c15-14(16,17)10-4-12(20)22-11-3-7(1-2-9(10)11)18-13(21)19-8-5-23-24-6-8/h1-4,8H,5-6H2,(H2,18,19,21)
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| Chemical Name |
1-(dithiolan-4-yl)-3-[2-oxo-4-(trifluoromethyl)chromen-7-yl]urea
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 100 mg/mL (265.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.64 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (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.
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