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环丙贝特

环丙贝特用途

Ciprofibrate是PPAR激动剂。

环丙贝特名称

[ CAS 号 ]:
52214-84-3

[ 中文名 ]:
环丙贝特

[ 英文名 ]:
Ciprofibrate

[中文别名 ]:

氯环丙妥明

[英文别名 ]:

Ciprofibrate
EINECS 257-744-6
MFCD00467135
UNII:F8252JGO9S

环丙贝特生物活性

[ 描述 ]:

Ciprofibrate是PPAR激动剂。

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

PPARα

[参考文献]

[1]. Passilly, P., et al., Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate. Biochem Pharmacol, 1999. 58(6): p. 1001-8.

[2]. Clemencet, M.C., et al., Differences in cell proliferation in rodent and human hepatic derived cell lines exposed to ciprofibrate. Cancer Lett, 2005. 222(2): p. 217-26.

[相关活性小分子]

环丙贝特物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
424.9±45.0 °C at 760 mmHg

[ 熔点 ]:
114 - 118ºC

[ 分子式 ]:
C₁₃H₁₄Cl₂O₃

[ 分子量 ]:
289.155

[ 闪点 ]:
210.7±28.7 °C

[ 精确质量 ]:
288.032013

[ PSA ]:
46.53000

[ LogP ]:
2.87

[ 外观性状 ]:
白色或近乎于白色结晶粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.579

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
可溶于：甲醇

环丙贝特MSDS

环丙贝特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UF0880000

CHEMICAL NAME :: Propionic acid, 2-(4-(2,2-dichlorocyclopropyl)phenoxy)-2-methyl-

CAS REGISTRY NUMBER :: 52214-84-3

LAST UPDATED :: 199706

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C13-H14-Cl2-O3

MOLECULAR WEIGHT :: 289.17

WISWESSER LINE NOTATION :: L3TJ AG AG BR DOX1&1&VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3640 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other oxidoreductases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 105 mg/kg/7D-C

TOXIC EFFECTS :: Liver - other changes Liver - changes in liver weight Biochemical - Metabolism (Intermediary) - other proteins

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 mg/kg/5D-I

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 14560 mg/kg/26W-I

TOXIC EFFECTS :: Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6390 mg/kg/60W-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors Lungs, Thorax, or Respiration - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6720 mg/kg/64W-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7300 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Gastrointestinal - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 280 mg/kg

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

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

TYPE OF TEST :: Morphological transformation

TYPE OF TEST :: DNA damage

TYPE OF TEST :: Unscheduled DNA synthesis

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - rat Liver

DOSE/DURATION :: 100 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 286,135,1993

环丙贝特安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H350

[ 警示性声明 ]:
P201-P280-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R45

[ 安全声明 (欧洲) ]:
S53-S22-S36/37/39-S45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UF0880000

[ 海关编码 ]:
2918990090

环丙贝特合成路线

环丙贝特上下游产品

环丙贝特上游产品

环丙贝特下游产品

环丙贝特制备

在0℃将8g(0.0356mo1)4-(2，2-二氯环丙基)苯酚、11.2g(0.28mol)固体氢氧化钠、11g氯仿和350ml丙酮的混合。移去冷浴，搅拌片刻后，再在蒸汽浴上加热至回流。搅拌回流3h后，真空浓缩。剩余液用稀碳酸氢钠水溶液和乙醚进行分配。碳酸氢钠溶液用浓盐酸酸化后，用乙醚提取。提取液用无水硫酸钠干燥，浓缩。黄色的油状剩余液(9.5g)用己烷重结晶2次，得6.0g淡奶油色的环丙贝特固体，熔点114-116℃。

环丙贝特海关

[ 海关编码 ]: 2918990090

[ 中文概述 ]:
2918990090. 其他含其他附加含氧基羧酸（包括酸酐、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:13.0%. 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 ]:
2918990090. other carboxylic acids with additional oxygen function and their anhydrides, halides, peroxides and peroxyacids; their halogenated, sulphonated, nitrated or nitrosated derivatives. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

环丙贝特文献

Transcriptional Regulation of Cytosolic Sulfotransferase 1C2 by Intermediates of the Cholesterol Biosynthetic Pathway in Primary Cultured Rat Hepatocytes.

J. Pharmacol. Exp. Ther. 355 , 429-41, (2015)

Cytosolic sulfotransferase 1C2 (SULT1C2) is expressed in the kidney, stomach, and liver of rats; however, the mechanisms regulating expression of this enzyme are not known. We evaluated transcriptiona...

Ciprofibrate increases cholesteryl ester transfer protein gene expression and the indirect reverse cholesterol transport to the liver.

Lipids Health Dis. 8 , 50, (2009)

CETP is a plasma protein that modulates atherosclerosis risk through its HDL-cholesterol reducing action. The aim of this work was to examine the effect of the PPARalpha agonist, ciprofibrate, on the ...

Ciprofibrate, clofibric acid and respective glycinate derivatives. Effects of a four-week treatment on male lean and obese Zucker rats.

Arzneimittelforschung 58(5) , 225-41, (2008)

Fibrates are widely prescribed in hyperlpidemic patients to prevent atherosclerosis. Their therapeutic use, however, can be associated with adverse effects like gastrointestinal disorders, myalgia, my...

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