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氟康唑

氟康唑用途

Fluconazole是抗真菌化合物,可用于表面和全身性的真菌感染。

氟康唑名称

[ CAS 号 ]:
86386-73-4

[ 中文名 ]:
氟康唑

[ 英文名 ]:
Fluconazole

[中文别名 ]:

[英文别名 ]:

triflucan
Flunazol
Apo Fluconazole
FluMycon
Zonal
Apo-Fluconazole
Diflucan
Zoltec
Difluean
Fluconazole

氟康唑生物活性

[ 描述 ]:

Fluconazole是抗真菌化合物,可用于表面和全身性的真菌感染。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

[参考文献]

[1]. Odds, F.C., S.L. Cheesman, and A.B. Abbott, Antifungal effects of fluconazole (UK 49858), a new triazole antifungal, in vitro. J Antimicrob Chemother, 1986. 18(4): p. 473-8.

[2]. Molgaard-Nielsen, D., B. Pasternak, and A. Hviid, Use of oral fluconazole during pregnancy and the risk of birth defects. N Engl J Med, 2013. 369(9): p. 830-9.

[3]. Black, L.A., et al., Pharmacokinetics of fluconazole following intravenous and oral administration to koalas (Phascolarctos cinereus). J Vet Pharmacol Ther, 2013.

[相关活性小分子]

氟康唑物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
579.8±60.0 °C at 760 mmHg

[ 熔点 ]:
138-140°C

[ 分子式 ]:
C₁₃H₁₂F₂N₆O

[ 分子量 ]:
306.271

[ 闪点 ]:
304.4±32.9 °C

[ 精确质量 ]:
306.104065

[ PSA ]:
81.65000

[ LogP ]:
0.50

[ 外观性状 ]:
白色或灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.663

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
DMSO: 5 mg/mL

氟康唑MSDS

氟康唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XZ4810000

CHEMICAL NAME :: 1H-1,2,4-Triazole-1-ethanol, alpha-(2,4-difluorophenyl)-alpha-(1H-1,2,4-triazol-1- ylmethyl)-

CAS REGISTRY NUMBER :: 86386-73-4

LAST UPDATED :: 199609

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C13-H12-F2-N6-O

MOLECULAR WEIGHT :: 306.31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1456 mg/kg/26W-I

TOXIC EFFECTS :: Skin and Appendages - hair

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 123,354,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1040 mg/kg/26W-I

TOXIC EFFECTS :: Skin and Appendages - hair

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 123,354,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 60 mg/kg/3W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - changes in potassium Nutritional and Gross Metabolic - other changes

REFERENCE :: PGMJAO Postgraduate Medical Journal. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.1- 1925- Volume(issue)/page/year: 67,1084,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1271 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >941 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 29,161,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1408 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1273 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 29,161,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,983,1990

氟康唑安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
XZ4810000

[ 海关编码 ]:
2933990090

氟康唑合成路线

氟康唑上下游产品

氟康唑上游产品

氟康唑下游产品

氟康唑制备

方法1：从甲酰胺、水合肼和85％甲酸可得1H-1，2，4-三唑。从间苯二胺可得间二氟苯，再溴化得2，4-二氟溴苯。镁溶于无水乙醚中，在超声波辐射下滴加2，4-二氟溴苯的乙醚溶液，然后在冰浴冷却下滴加1，3-二氯丙酮的乙醚溶液，室温搅拌过夜。加入冰醋酸和水。分出的有机层干燥后浓缩。浓缩液和三唑、碳酸钾、PEG600溶于干燥乙酸乙酯中，回流。过滤，水洗至中性，干燥。蒸除溶剂，乙酸乙酯一环己烷(1：1)重结晶，得氟康唑，总收率33.6%，熔点138.5-140℃。

最后一步也可在丙腈中进行。1，3-二卤(x=Br或Cl)-2-(2，4-二氟苯基)-2-丙醇和1H-1，2，4-三唑在丙腈中，氢氧化钠催化及PEG 600相转移催化下回流，可得氟康唑粗品。该粗品溶于脂肪醇(如丙醇、异丙醇或丁醇等)，加热溶解，用少量活性炭脱色后，冷却得结晶，即为氟康唑精品，熔点139～140℃。

方法2:2，4-二氟苯甲酸甲酯和1-氯甲基-1，2，4-三氮唑的格氏试剂反应，并水解即可得到氟康唑。

方法3：二氟苯经溴化生成1-溴-2，4-二氟苯，再转化为其格氏试剂。

上述得到的格氏试剂和1，3-双(1H-1,2,4-三氮唑基)丙酮反应，接着水解即可得到氟康唑

氟康唑海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氟康唑文献

Antifungal susceptibility and virulence attributes of animal-derived isolates of Candida parapsilosis complex.

J. Med. Microbiol. 63(Pt 11) , 1568-72, (2014)

This study aimed to identify strains of the Candida parapsilosis complex isolated from animals, as well as to assess their in vitro antifungal susceptibility profile and in vitro production of virulen...

Simultaneous determination of seven azole antifungal drugs in serum by ultra-high pressure liquid chromatography and diode array detection.

Acta Clin. Belg. 69(1) , 53-61, (2014)

Azole antifungals are a group of fungistatic agents that can be administered orally or parenterally. The determination of the concentrations of these antifungals (miconazole, fluconazole, ketoconazole...

Prophylactic oral/topical non-absorbed antifungal agents to prevent invasive fungal infection in very low birth weight infants.

Cochrane Database Syst. Rev. 3 , CD003478, (2013)

Invasive fungal infection is an important cause of mortality and morbidity in very preterm or very low birth weight infants. Uncertainty exists about the effect of prophylactic oral/topical non-absorb...

更多文献

氟康唑相关知识

[氟康唑胶囊] - 说明书 - 作用 - 氟康唑副作用

2018-12-15 20:09:34

导读：氟康唑（英语：Fluconazole）是一种三唑，可用于医治由真菌引起的病征。常见的商品名称有大扶康（Diflucan）或“Trican”（辉瑞）。在墨西哥的药店则以“Alfumet”为名销售。【药品名称】通用名称：氟康唑胶囊商品名称：氟康唑胶囊(大扶康) 英文名称：Flucona...

氟康唑