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氯贝特

氯贝特用途

Clofibrate 是 PPAR 的激动剂,对人和鼠 PPARα 和 PPARγ 的 EC50 值分别为 55 μM,∼500 μM 和 50 μM,∼500 μM。

氯贝特名称

[ CAS 号 ]:
637-07-0

[ 中文名 ]:
氯贝特

[ 英文名 ]:
clofibrate

[中文别名 ]:

[英文别名 ]:

ethyl 2-[(4-chlorophenyl)oxy]-2-methylpropanoate
MFCD00000615
Ethyl α-(p-chlorophenoxy)isobutyrate
Ethyl p-chlorophenoxyisobutyrate
Ethyl α-(4-chlorophenoxy)isobutyrate
Clofipront
Clofibric Acid, Ethyl Ester
2-(p-chlorophenoxy)isobutyric acid ethyl ester
Ethyl α-(4-chlorophenoxy)-α-methylpropionate
clofibrate

氯贝特生物活性

[ 描述 ]:

Clofibrate 是 PPAR 的激动剂,对人和鼠 PPARα 和 PPARγ 的 EC50 值分别为 55 μM,∼500 μM 和 50 μM,∼500 μM。

[ 相关类别 ]:

研究领域 >> 代谢疾病

[ 靶点 ]

PPARα:50 μM (EC50)

PPARγ:500 μM (EC50)

[体外研究]

Clofibrate是一种PPAR激动剂,对于小鼠PPARα和PPARγ,E50s分别为50μM,~500μM,人PPARα和PPARγ分别为55μM,~500μM[1]。氯贝特(0.5,1,2mM)增加两种脂肪酸(FA)处理的大鼠肝细胞瘤细胞中的FABP1表达。 Clofibrate在早期治疗后降低ROS水平,远远超过FA治疗细胞的晚期治疗[2]。

[体内研究]

Clofibrate(0.5％)上调胎儿血清浓度和FGF21的肝脏表达,停用氯贝特后停用基础水平。 Clofibrate给药后代在腹股沟脂肪中对HFD的反应具有显着更高的产热基因(Ucp1,Cidea,Ppara Ppargc1a,Cpt1b)和UCP1蛋白水平的表达,但在腹膜后(与肾周)或附睾脂肪组合中没有[3]。

[细胞实验]

将细胞以2.5×10 4个细胞/孔的密度接种（用于WST-1，细胞内脂滴定量和二氯荧光素（DCF）测定，96孔板）和1×10 5个细胞/孔（用于尼罗红染色，12-在MEM / EBSS培养基中培养板，并孵育过夜以进行粘附。第二天，细胞培养基用新鲜制备的培养基替换，该培养基含有脂肪酸混合物油酸盐：棕榈酸酯（2：1），在不含3％脂肪酸的牛血清白蛋白存在下。将细胞用0,0.5,1,2和3mM脂肪酸（FA）混合物在37℃下在湿润的培养箱中在95％空气和5％CO 2的气氛中处理24和48小时。氯贝特用于增加处理的细胞培养物中FABP1的水平。将氯贝特（500μM）溶解在DMSO中，然后加入到培养基中（DMSO <0.1％v / v，终体积）。将对照细胞与单独的DMSO一起温育。四种不同的细胞治疗包括1天FA治疗，2天FA治疗，早期氯贝特干预和晚期氯贝特干预[1]。

[动物实验]

雌性和雄性C57BL / 6JNarl小鼠用于育种。使用具有1至5的奇偶性的女性。从育种到分娩，给怀孕的雌性喂食对照（C）或实验（CF）饮食。 C饮食基于AIN-93M饮食，略微改变以含有来自大豆油的21kcal％脂肪，而CF饮食是添加0.5％氯贝特的C饮食。怀孕是由于阴道栓（定义为妊娠第1天）的存在。自发分娩后（妊娠日19.5±0.5），所有同窝仔畜均由饲喂C饮食3天的大坝均匀饲养，产仔数调整至8-10，断奶至非纯化标准饮食4周，然后换成a HFD（51千卡脂肪，基于黄油）5周。在这项研究中，根据母亲的饮食（C或CF），仅使用雄性后代和2组后代。将所有小鼠保持在维持在23±2℃的房间中，具有受控的12小时光照： - 暗淡循环，随意进食和饮用水。每周记录体重和采食量[3]。

[参考文献]

[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.

[2]. Chen Y, et al. Clofibrate Attenuates ROS Production by Lipid Overload in Cultured Rat Hepatoma Cells. J Pharm Pharm Sci. 2017;20(0):239-251.

[3]. Chen SH, et al. Prenatal PPARα activation by clofibrate increases subcutaneous fat browning in male C57BL/6J mice fed a high-fat diet during adulthood. PLoS One. 2017 Nov 2;12(11):e0187507.

[相关活性小分子]

氯贝特物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
274.8±0.0 °C at 760 mmHg

[ 分子式 ]:
C₁₂H₁₅ClO₃

[ 分子量 ]:
242.699

[ 闪点 ]:
115.1±19.9 °C

[ 精确质量 ]:
242.070969

[ PSA ]:
35.53000

[ LogP ]:
3.32

[ 外观性状 ]:
透明无色油状

[ 蒸汽压 ]:
0.0±0.5 mmHg at 25°C

[ 折射率 ]:
1.505

[ 储存条件 ]:
通风低温干燥

氯贝特MSDS

详细MSDS(安全技术说明书)

氯贝特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UE9480000

CHEMICAL NAME :: Propionic acid, 2-(p-chlorophenoxy)-2-methyl-, ethyl ester

CAS REGISTRY NUMBER :: 637-07-0

BEILSTEIN REFERENCE NO. :: 1913459

LAST UPDATED :: 199706

DATA ITEMS CITED :: 51

MOLECULAR FORMULA :: C12-H15-Cl-O3

MOLECULAR WEIGHT :: 242.72

WISWESSER LINE NOTATION :: GR DOX1&1&VO2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 4232 mg/kg/57W-I

TOXIC EFFECTS :: Behavioral - muscle weakness Behavioral - muscle contraction or spasticity Musculoskeletal - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1071 ug/kg

TOXIC EFFECTS :: Behavioral - tremor

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 80 mg/kg/2D-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - body temperature increase

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 171 mg/kg/6D-I

TOXIC EFFECTS :: Behavioral - muscle weakness Musculoskeletal - other changes

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 940 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 910 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1220 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 540 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >500 mg/kg

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

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1370 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 1280 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 2400 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 1260 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 3 gm/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7 gm/kg/14D-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 transferases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3750 mg/kg/30D-C

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 gm/kg/4W-I

TOXIC EFFECTS :: Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14700 mg/kg/7W-C

TOXIC EFFECTS :: Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - catalases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1698 mg/kg/6D-C

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 7 gm/kg/14D-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 - other transferases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 gm/kg/72W-C

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1050 mg/kg

SEX/DURATION :: female 16-22 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 14 gm/kg

SEX/DURATION :: female 2 week(s) pre-mating - 3 week(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 gm/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3960 mg/kg

SEX/DURATION :: male 22 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 960 mg/kg

SEX/DURATION :: female 17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - biochemical and metabolic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 1440 mg/kg

SEX/DURATION :: female 14-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1300 mg/kg

SEX/DURATION :: female 6-18 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

TYPE OF TEST :: DNA damage

TYPE OF TEST :: Unscheduled DNA synthesis

TYPE OF TEST :: Unscheduled DNA synthesis

TYPE OF TEST :: Unscheduled DNA synthesis

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 100 umol/L/1H

REFERENCE :: CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 5,703,1984 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,39,1980 IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,391,1996 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,39,1980 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,391,1996 IARC Cancer Review:Group 3 IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,391,1996 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - T0426 No. of Facilities: 28 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 4648 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - T0426 No. of Facilities: 33 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 323 (estimated) No. of Female Employees: 176 (estimated)

氯贝特安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H318-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R40

[ 安全声明 (欧洲) ]:
S26-S36/37/39-S61-S45-S36/37

[ 危险品运输编码 ]:
UN 3082 9/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
UE9480000

[ 海关编码 ]:
2918990090

氯贝特上下游产品

氯贝特上游产品

氯贝特下游产品

氯贝特制备

按照采用的原料划分，该品合格路线主要有两条，一是以对氨基苯酚为原料经重氮化；置换制得对氯苯酚，再经缩合；水解，酸化生成对氯苯氧异丁酸，最后酯化得安妥明。这条路线步骤较长，所用原料对氨基酚不稳定，但比较成熟。二是以苯酚为原料，经缩合生成苯氧异丁酸，再于乙醇中通氯，进行氯化及酯化反应生成安妥明。

氯贝特海关

[ 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%

氯贝特文献

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

The Japanese toxicogenomics project: application of toxicogenomics.

Mol. Nutr. Food. Res. 54 , 218-27, (2010)

Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted appr...

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氯贝特