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伊洛前列素

伊洛前列素用途

Iloprost (ZK 36374)是一种前列环素PGI2的合成类似物。

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伊洛前列素名称

[ CAS 号 ]:
78919-13-8

[ 中文名 ]:
伊洛前列素

[ 英文名 ]:
Iloprost

[英文别名 ]:

CILOPROST
Iloprost
Ataprostum [INN-Latin]
Ataprost
Ataprostum
Ataprost [INN]

伊洛前列素生物活性

[ 描述 ]:

Iloprost (ZK 36374)是一种前列环素PGI2的合成类似物。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

研究领域 >> 内分泌

[参考文献]

[1]. Della Bella S, et al. Novel mode of action of iloprost: in vitro down-regulation of endothelial cell adhesion molecules. Prostaglandins Other Lipid Mediat. 2001 Jun;65(2-3):73-83.

[2]. van der Giessen WJ, et al. The effect of the stable prostacyclin analogue ZK 36374 on experimental coronary thrombosis in the pig. Thromb Res. 1984 Oct 1;36(1):45-51.

[3]. Addonizio VP Jr, et al. Prevention of heparin-induced thrombocytopenia during open heart surgery with iloprost (ZK36374). Surgery. 1987 Nov;102(5):796-807.

[相关活性小分子]

伊洛前列素物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
539.2±50.0 °C at 760 mmHg

[ 熔点 ]:
115.7ºC

[ 分子式 ]:
C₂₂H₃₂O₄

[ 分子量 ]:
360.487

[ 闪点 ]:
294.0±26.6 °C

[ 精确质量 ]:
360.230072

[ PSA ]:
77.76000

[ LogP ]:
2.94

[ 外观性状 ]:
无色油状

[ 蒸汽压 ]:
0.0±3.3 mmHg at 25°C

[ 折射率 ]:
1.629

[ 储存条件 ]:
Desiccate at -20°C

伊洛前列素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SA3695000

CHEMICAL NAME :: Pentanoic acid, 5-(hexahydro-5-hydroxy-4-(3-hydroxy-4-methyl-1-octen- 6-ynyl)-2(1H)- pentalenylidene)-

CAS REGISTRY NUMBER :: 78919-13-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C22-H32-O4

MOLECULAR WEIGHT :: 360.54

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >100 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 6,676,1981

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 119 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 4,209,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >100 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 6,676,1981

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 201 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 4,209,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21780 ug/kg/11D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Blood - other changes

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 4,209,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 120 mg/kg/28D-C

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 4,209,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 4760 ug/kg/28D-C

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Vascular - BP lowering not characterized in autonomic section Related to Chronic Data - death

REFERENCE :: NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 4,209,1986 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 10 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 78,223,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 26100 ug/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 22 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 78,223,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 26100 ug/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 22 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: TOLED5 Toxicology Letters. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1977- Volume(issue)/page/year: 78,223,1995

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伊洛前列素安全信息

[ 海关编码 ]:
2918199090

伊洛前列素合成路线

详细合成路线

伊洛前列素上下游产品

伊洛前列素上游产品

伊洛前列素下游产品

伊洛前列素制备

由化合物(I)出发，经中间体Ⅱ得到伊洛前列素。

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伊洛前列素海关

[ 海关编码 ]: 2918199090

[ 中文概述 ]:
HS: 2918199090. 其他含醇基但不含其他含氧基羧酸（包括其酸酐、酰卤化物、过氧化物和过氧酸及该税号的衍生物）. 增值税率:17.0%. 退税率:9.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2918199090 other carboxylic acids with alcohol function but without other oxygen function, their anhydrides, halides, peroxides, peroxyacids and their derivatives。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%

伊洛前列素

伊洛前列素用途

伊洛前列素名称

伊洛前列素生物活性

伊洛前列素物理化学性质

伊洛前列素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

伊洛前列素安全信息

伊洛前列素合成路线

详细合成路线

伊洛前列素上下游产品

伊洛前列素上游产品

伊洛前列素下游产品

伊洛前列素制备

伊洛前列素海关

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