| 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 |
EFC targets CYP enzymes, including CYP2B6, CYP1A1, CYP1A2, and CYP2C isoforms, which catalyze its O-deethylation. The compound does not target a single receptor but instead serves as a probe substrate for CYP-mediated oxidative metabolism.
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| ln Vitro |
In cell-free CYP enzyme assays, EFC is rapidly O-deethylated by CYPs to produce the highly fluorescent metabolite 7-hydroxy-4-trifluoromethylcoumarin (HFC). The fluorescence increase correlates directly with CYP activity. Ex/Em maxima of HFC: 410/510 nm. The probe is selective for specific CYP isoforms depending on assay conditions and enzyme sources.
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| ln Vivo |
No classical in vivo activity data are documented as EFC is a probe substrate for measuring CYP enzyme activity, not a pharmacologically active compound for systemic administration. Its utility lies exclusively in detecting and quantifying enzyme function in vitro and ex vivo.
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| Enzyme Assay |
This cell-free assay is performed using recombinant human CYP enzymes or human liver microsomes. EFC (1-200 uM) is incubated with NADPH-regenerating system in assay buffer at 37degC. The reaction is terminated by adding stop solution (ice-cold acetonitrile or NaOH). The product HFC is quantified fluorometrically (Ex/Em 410/510 nm). Kinetic parameters (Km, Vmax) are calculated from Michaelis-Menten analysis.
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| Cell Assay |
Cell lines expressing specific CYP isoforms (e.g., CYP2B6-transfected cells) or primary human hepatocytes are incubated with EFC (10-100 uM) in culture medium for 30-60 min at 37degC. HFC accumulation in the medium or cell lysates is measured fluorometrically to assess cellular CYP activity. For CYP inhibition studies, test compounds are co-incubated with EFC and residual activity is calculated relative to controls.
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| Animal Protocol |
CYP enzymes in liver microsomes or S9 fractions from treated animals are incubated with EFC and NADPH, and HFC fluorescence is measured to assess changes in CYP activity following drug treatment or disease states. EFC is not administered to live animals; rather, tissues are collected post-treatment for ex vivo activity measurements.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
7-Ethoxy-4-trifluoromethylcoumarin's known human metabolites include 7-hydroxy-4-trifluoromethylcoumarin. EFC has no therapeutic pharmacokinetic properties as it is a probe substrate for enzyme activity assays, not a drug candidate. For research use, stock solutions are prepared in DMSO (100 mg/mL, 316.11 mM). The compound is stable as a powder at -20degC for 3 years and as a solution at -80degC for 6 months. Ex/Em: 410/510 nm. |
| Toxicity/Toxicokinetics |
Standard laboratory safety precautions apply. EFC is a fluorogenic probe for research use only. Avoid inhalation, ingestion, and skin contact. Use personal protective equipment. The compound should be stored protected from light and moisture to maintain stability. For disposal, follow institutional guidelines for chemical waste.
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| References | |
| Additional Infomation |
This is a research-use-only fluorogenic substrate, not an approved pharmaceutical. It is used to characterize CYP enzyme kinetics, screen for CYP inhibition or induction, and study drug-drug interactions in drug discovery and development. Molecular formula: C12H9F3O3; molecular weight: 258.19. Metabolite: 7-Hydroxy-4-trifluoromethylcoumarin (HFC).
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| Molecular Formula |
C12H9O3F3
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|---|---|
| Molecular Weight |
258.19326
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| Exact Mass |
258.05
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| CAS # |
115453-82-2
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| PubChem CID |
130779
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| Appearance |
Off-white to pink solid powder
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| Density |
1.368 g/cm3
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| Boiling Point |
303.1ºC at 760 mmHg
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| Flash Point |
132.7ºC
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| Vapour Pressure |
0.000952mmHg at 25°C
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| Index of Refraction |
1.503
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| LogP |
3.21
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
362
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OLHOIERZAZMHGK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H9F3O3/c1-2-17-7-3-4-8-9(12(13,14)15)6-11(16)18-10(8)5-7/h3-6H,2H2,1H3
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| Chemical Name |
7-ethoxy-4-(trifluoromethyl)chromen-2-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.8731 mL | 19.3656 mL | 38.7312 mL | |
| 5 mM | 0.7746 mL | 3.8731 mL | 7.7462 mL | |
| 10 mM | 0.3873 mL | 1.9366 mL | 3.8731 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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