<生产厂家价格>

伊曲康唑

伊曲康唑用途

Itraconazole是抗真菌剂。

伊曲康唑名称

[ CAS 号 ]:
84625-61-6

[ 中文名 ]:
伊曲康唑

[ 英文名 ]:
Itraconazole

[中文别名 ]:

[英文别名 ]:

Itrizole
Candistat
Sporanos
MFCD08064196
Itrac
Cladosal 100
Canditral
Itraconazole

伊曲康唑生物活性

[ 描述 ]:

Itraconazole是抗真菌剂。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 抗感染 >> 真菌

研究领域 >> 感染

[参考文献]

[1]. Kim, J., et al., Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell, 2010. 17(4): p. 388-99.

[2]. Chong, C.R., et al., Inhibition of angiogenesis by the antifungal drug itraconazole. ACS Chem Biol, 2007. 2(4): p. 263-70.

[3]. Shi, W., et al., Itraconazole side chain analogues: structure-activity relationship studies for inhibition of endothelial cell proliferation, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, and hedgehog signaling. J Med Chem, 2011. 54(20): p. 7363-74.

[4]. Olkkola, K.T., J.T. Backman, and P.J. Neuvonen, Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole. Clinical Pharmacology & Therapeutics, 1994. 55(5): p. 481-485.

[相关活性小分子]

伊曲康唑物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
850.0±75.0 °C at 760 mmHg

[ 熔点 ]:
166°C

[ 分子式 ]:
C₃₅H₃₈Cl₂N₈O₄

[ 分子量 ]:
705.633

[ 闪点 ]:
467.9±37.1 °C

[ 精确质量 ]:
704.239319

[ PSA ]:
104.70000

[ LogP ]:
4.35

[ 外观性状 ]:
灰白色结晶固体

[ 蒸汽压 ]:
0.0±3.2 mmHg at 25°C

[ 折射率 ]:
1.678

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
chloroform: 50 mg/mL, clear, colorless

伊曲康唑MSDS

伊曲康唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XZ5481000

CHEMICAL NAME :: 3H-1,2,4-Triazol-3-one, 4-(4-(4-(4-((2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triaz ol-1-ylmethyl)- 1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazinyl)pheny l)-2,4-dihydro-2-(1-m ethylpropyl)-

CAS REGISTRY NUMBER :: 84625-61-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C35-H38-Cl2-N8-O4

MOLECULAR WEIGHT :: 705.71

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 32 mg/kg/8D-I

TOXIC EFFECTS :: Skin and Appendages - hair

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 293,822,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 140 mg/kg/5W-I

TOXIC EFFECTS :: Liver - jaundice, other or unclassified Liver - liver function tests impaired Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,251,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 240 mg/kg/6W-I

TOXIC EFFECTS :: Liver - jaundice, other or unclassified Liver - liver function tests impaired

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,251,1992

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >320 mg/kg

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

REFERENCE :: RINDDG Reviews of Infectious Diseases. (University of Chicago Press, Journals Division, POB 37005, Chicago, IL. 60637) V.1- 1979- Volume(issue)/page/year: 9(Suppl 1),S43,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 40 mg/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,381,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >320 mg/kg

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

REFERENCE :: RINDDG Reviews of Infectious Diseases. (University of Chicago Press, Journals Division, POB 37005, Chicago, IL. 60637) V.1- 1979- Volume(issue)/page/year: 9(Suppl 1),S43,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 46400 ug/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,381,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >200 mg/kg

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

REFERENCE :: RINDDG Reviews of Infectious Diseases. (University of Chicago Press, Journals Division, POB 37005, Chicago, IL. 60637) V.1- 1979- Volume(issue)/page/year: 9(Suppl 1),S43,1987

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >160 mg/kg

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

REFERENCE :: RINDDG Reviews of Infectious Diseases. (University of Chicago Press, Journals Division, POB 37005, Chicago, IL. 60637) V.1- 1979- Volume(issue)/page/year: 9(Suppl 1),S43,1987 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 29120 mg/kg/1Y-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Metabolism (Intermediary) - lipids including transport Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,381,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14560 mg/kg/13W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Related to Chronic Data - death Related to Chronic Data - changes in ovarian weight

REFERENCE :: RINDDG Reviews of Infectious Diseases. (University of Chicago Press, Journals Division, POB 37005, Chicago, IL. 60637) V.1- 1979- Volume(issue)/page/year: 9(suppl 1),S43,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 7280 mg/kg/91D-C

TOXIC EFFECTS :: Liver - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,381,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 29120 mg/kg/1Y-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - changes in calcium Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,381,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1760 mg/kg

SEX/DURATION :: female 8-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 25,381,1991

伊曲康唑安全信息

[ 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;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xi:Irritant

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S22-S26-S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
XZ5481000

[ 海关编码 ]:
2934999090

伊曲康唑合成路线

伊曲康唑上下游产品

伊曲康唑上游产品

伊曲康唑下游产品

伊曲康唑制备

从间二氯苯出发，经和酮康唑完全相似的反应可得到化合物(I)。化合物(Ⅰ)再和1-乙酰基-4-(4-羟基苯基)哌嗪缩合，接着水解脱去乙酰基，和对硝基氯苯缩合，氢化还原，氯甲酸酯酰化，然后和水合肼反应后再环合，烷基化得伊曲康唑。其中间体1-乙酰基-4-(4-羟基苯基)哌嗪可以哌嗪为原料，经下面的反应来制备。

伊曲康唑海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

伊曲康唑文献

Itraconazole suppresses the growth of glioblastoma through induction of autophagy: involvement of abnormal cholesterol trafficking.

Autophagy 10(7) , 1241-55, (2014)

Glioblastoma is one of the most aggressive human cancers with poor prognosis, and therefore a critical need exists for novel therapeutic strategies for management of glioblastoma patients. Itraconazol...

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...

European Confederation of Medical Mycology (ECMM) epidemiological survey on invasive infections due to Fusarium species in Europe.

Eur. J. Clin. Microbiol. Infect. Dis. 33(9) , 1623-30, (2014)

In order to better understand the epidemiology of fusariosis in Europe, a survey collecting information on the clinical characteristics of the patients infected by Fusarium as well as on the infecting...

更多文献