| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| 体外研究 (In Vitro) |
氟康唑抑制四种烟曲霉，IC50 为 23.9–43.5 μg/mL。在添加血清的培养基中，氟康唑 (0.20 μg/mL) 会强烈抑制白色念珠菌的菌丝体阶段发育和芽管伸长 [1]。氟康唑是一种三唑类抗真菌药物，可预防隐球菌和念珠菌引起的感染。针对克柔念珠菌和光滑念珠菌 (MIC ≥ 32 μg/mL) 的 MIC90 最大 (MIC > 64 μg/mL)。对于以下念珠菌属物种，MIC 小于 2 μg/mL：白色念珠菌 C. 0.5 μg/mL、近平滑念珠菌 C. 2 μg/mL、热带念珠菌 (2 μg/mL)。 C. lusitaniae (2 μg/mL)。 0.5 μg/mL 开菲尔 [2]。药物氟康唑 (0.1–50.0 μg/mL) 可杀死真菌细胞并降低其活力 [3]。
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| 体内研究 (In Vivo) |
在全身性念珠菌病小鼠模型中，氟康唑（0、0.5、1、2.5、5、7.5 和 10 mg/kg；腹膜内 (ip) 单剂量）使真菌密度 (ED50) 降低 50%，至 4.87 mg/kg。 4]。腹腔注射后氟康唑的终末消除半衰期为 2.4 小时。氟康唑的给药量对终末半衰期没有影响[4]。
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| 细胞实验 |
细胞活力测定[3]
细胞类型：白色念珠菌酵母细胞（菌株 ATCC 26310 和菌株 TW） 测试浓度： 0.1、0.5、5.0 , 50.0 μg/mL 孵育时间：24 小时 实验结果：针对两种菌株的 MIC 均为 0.5 μg/mL。 |
| 动物实验 |
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 |
| 参考文献 |
[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. |
| 分子式 |
C13H12F2N6O
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|---|---|---|
| 分子量 |
306.27
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| CAS号 |
86386-73-4
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| 相关CAS号 |
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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| 化学名 |
2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-ol
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| 别名 |
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
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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| 溶解度 (体外) |
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| 溶解度 (体内) |
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). 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| 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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