| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Fungal cytochrome P450 14alpha-demethylase (CYP51); inhibits ergosterol synthesis, disrupting fungal cell membrane integrity.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Unlabeled Efinaconazole is a broad-spectrum triazole antifungal agent with potent activity against dermatophytes, Candida, and Malassezia species. It inhibits T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 microg/mL and 0.00098 microg/mL, respectively. |
| ln Vivo |
Unlabeled Efinaconazole is clinically used as a topical antifungal for the treatment of onychomycosis (toenail fungus). It is effective in clearing fungal infections with once-daily application for up to 48 weeks. The d4-labeled analog is used only for internal standardization.
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| Enzyme Assay |
Not applicable; antifungal activity is assessed in broth microdilution assays (CLSI M38/M27), not in enzyme/receptor binding assays. The d4-labeled compound serves as an internal standard in analytical methods.
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| Cell Assay |
Fungal strains (dermatophytes, Candida spp.) are cultured in RPMI-1640 medium; MIC is determined by broth microdilution according to CLSI guidelines. For analytical protocols, Efinaconazole-d4 is used as internal standard in LC-MS/MS quantification of unlabeled drug in biological samples.
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| Animal Protocol |
Animals are administered unlabeled Efinaconazole; plasma, nail, or tissue samples are collected; samples are extracted with organic solvent, spiked with Efinaconazole-d4 as internal standard, and analyzed by LC-MS/MS to quantify drug concentrations.
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| ADME/Pharmacokinetics |
Identical to unlabeled Efinaconazole; topical application leads to minimal systemic absorption (<1%); high drug concentrations are achieved in nail plates and keratin; plasma levels are very low; the d4 label does not alter PK properties.
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| Toxicity/Toxicokinetics |
No toxicity data for the d4 analog; Efinaconazole is well tolerated with minimal systemic toxicity due to low absorption; common adverse effects are mild local application site reactions (erythema, peeling, burning). No significant drug-drug interactions.
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| References |
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| Additional Infomation |
Efinaconazole (KP-103) is a triazole antifungal approved by FDA (brand name Jublia) and other regulatory agencies for the topical treatment of onychomycosis. The d4-labeled version is a research-grade analytical standard for LC-MS/MS quantification.
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| Molecular Formula |
C18H18D4F2N4O
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|---|---|
| Molecular Weight |
352.41
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| Related CAS # |
Efinaconazole;164650-44-6
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| Appearance |
White to off-white 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 |
| 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 | 2.8376 mL | 14.1880 mL | 28.3760 mL | |
| 5 mM | 0.5675 mL | 2.8376 mL | 5.6752 mL | |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8376 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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