Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Efinaconazole(formerly AGJ-95634; KP-103; CTK-5J2975; KB-145948; trade names Jublia; Clenafin) is a triazole antifungal drug approved for use in various countries such as the United States, Canada, and Japan as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nails). It acts as an inhibitor of 14α-demethylase, which is involved in the biosynthesis of ergosterol, a key constituent of fungal cell membranes.
ln Vivo |
Topical ifenconazole solution (0.25 to 1%) proved beneficial in treating interdigital tinea pedis and tinea corporis in ten guinea pigs in a dose-dependent manner. Thirty-day and nine-day follow-up investigations revealed that the recurrence rates of tinea corporis and tinea pedis in animals treated with 1% ifenconazole were thirty percent and twenty percent, respectively. Nine out of ten mice were protected against dermatophytosis when a single dosage of 1% ifuconazole was administered to the dorsal skin 48 hours prior to fungal inoculation, suggesting that active ifuconazole remains active after delivery and stays in skin tissue for at least 48 hours[2].
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References |
[1]. Tatsumi Y, et al. Mechanism of action of efinaconazole, a novel triazole antifungal agent. Antimicrob Agents Chemother. 2013 May;57(5):2405-9.
[2]. Tatsum Y, et al. KP-103, a novel triazole derivative, is effective in preventing relapse and successfully treating experimental interdigital tinea pedis and tinea corporis in guinea pigs. Microbiol Immunol. 2002;46(7):425-32. |
Molecular Formula |
C18H22F2N4O
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Molecular Weight |
348.39
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Exact Mass |
348.1762
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CAS # |
164650-44-6
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Related CAS # |
Efinaconazole-d4
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SMILES |
FC1C([H])=C(C([H])=C([H])C=1[C@@](C([H])([H])N1C([H])=NC([H])=N1)([C@@]([H])(C([H])([H])[H])N1C([H])([H])C([H])([H])C(=C([H])[H])C([H])([H])C1([H])[H])O[H])F
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Synonyms |
AGJ95634; KP103; CTK5J2975; KB145948; AGJ-95634; KP-103; CTK-5J2975; KB-145948; AGJ 95634; KP 103; CTK 5J2975; KB 145948; trade names Jublia; Clenafin
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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) |
DMSO : ≥ 100 mg/mL (~287.03 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.18 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.18 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 25.0 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: ≥ 2.5 mg/mL (7.18 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 | 2.8703 mL | 14.3517 mL | 28.7035 mL | |
5 mM | 0.5741 mL | 2.8703 mL | 5.7407 mL | |
10 mM | 0.2870 mL | 1.4352 mL | 2.8703 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.