| 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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Purity: ≥98%
Fluconazole (Diflucan, UK-49858; UK 49858; Triflucan, Elazor, Biozolene) is a novel, potent, and orally bioavailable triazole-based antifungal drug that works by inhibiting fungal lanosterol 14 alpha-demethylase-dependent biosynthesis of ergosterol, which is an essential component of fungal cell membrane.
| ln Vitro |
Four Aspergillus fumigatus species are inhibited by fluconazole, with an IC50 of 23.9–43.5 μg/mL. In serum-supplemented media, Candida albicans' mycelial stage development and germ tube elongation are strongly inhibited by fluconazole (0.20 μg/mL) [1]. Fluconazole is a triazole antifungal medication that prevents infections brought on by Cryptococcus and Candida. The greatest MIC90 (MIC > 64 μg/mL) is seen against Candida krusei and Candida glabrata (MIC ≥ 32 μg/mL). For the following species of Candida, the MIC is less than 2 μg/mL: C. 0.5 μg/mL of albicans, C. 2 μg/mL parapsilosis, C. C. tropicalis (2 μg/mL). C. lusitaniae (2 μg/mL). 0.5 μg/mL of kefyr [2]. The drug fluconazole (0.1–50.0 μg/mL) kills and diminishes the viability of fungus cells [3].
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| ln Vivo |
In a mouse model of systemic candidiasis, fluconazole (0, 0.5, 1, 2.5, 5, 7.5, and 10 mg/kg; intraperitoneal (ip) single dose) reduced fungal density (ED50) by 50% to 4.87 mg/kg[4]. Fluconazole has a 2.4-hour terminal elimination half-life following intraperitoneal injection. The amount of fluconazole given has no effect on the terminal half-life [4].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: C.albicans yeast cells (strain ATCC 26310 and strain TW) Tested Concentrations: 0.1, 0.5, 5.0, 50.0 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: The MICs against both strains were 0.5 μg/ mL. |
| Animal Protocol |
Animal/Disease Models: Female NYLAR mice (weight, 18 to 20 g; infected intravenously (iv)with C. albicans blastoconidia)[4]
Doses: 5, 10, 15 and 20 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Given ip as a single dose Experimental Results: T1/2=2.4 h |
| References |
[1]. H Yamaguchi, et al. [In vitro activity of fluconazole, a novel bistriazole antifungal agent]. Jpn J Antibiot. 1989 Jan;42(1):1-16.
[2]. M A Pfaller, et al. Interpretive breakpoints for fluconazole and Candida revisited: a blueprint for the future of antifungal susceptibility testing. Clin Microbiol Rev. 2006 Apr;19(2):435-47. [3]. P G Sohnle, et al. Effect of fluconazole on viability of Candida albicans over extended periods of time. Antimicrob Agents Chemother. 1996 Nov;40(11):2622-5. [4]. A Louie, et al. Pharmacodynamics of fluconazole in a murine model of systemic candidiasis. Antimicrob Agents Chemother. 1998 May;42(5):1105-9. |
| Molecular Formula |
C13H12F2N6O
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| Molecular Weight |
306.27
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| CAS # |
86386-73-4
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| Related CAS # |
Fluconazole-d4;1124197-58-5;Fluconazole hydrate;155347-36-7;Fluconazole mesylate;159532-41-9
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| SMILES |
FC1C([H])=C(C([H])=C([H])C=1C(C([H])([H])N1C([H])=NC([H])=N1)(C([H])([H])N1C([H])=NC([H])=N1)O[H])F
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| InChi Key |
RFHAOTPXVQNOHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12F2N6O/c14-10-1-2-11(12(15)3-10)13(22,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9,22H,4-5H2
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| Chemical Name |
2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-ol
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.16 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 (8.16 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 (8.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (6.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2651 mL | 16.3255 mL | 32.6509 mL | |
| 5 mM | 0.6530 mL | 3.2651 mL | 6.5302 mL | |
| 10 mM | 0.3265 mL | 1.6325 mL | 3.2651 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04122560 | Completed | Drug: Fluconazole 200mg tab Drug: Fluconazole 2 MG/ML |
Fluconazole Candidiasis |
Radboud University Medical Center | November 30, 2019 | Phase 4 |
| NCT04201054 | Completed | Drug: Fluconazole | Healthy Volunteers | Parc de Salut Mar | March 25, 2019 | Phase 1 |
| NCT03821480 | Completed | Drug: Test drug Drug: Reference drug |
Bioequivalence | Pfizer | January 28, 2019 | Phase 1 |
| NCT04038008 | Completed | Drug: Fluconazole Drug: Diflucan® |
Bioequivalence | Pharmtechnology LLC | July 26, 2019 | Phase 1 |
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