30299-08-2

• 常用中文名：克利贝特
• 常用英文名：Clinofibrate
• CAS号：30299-08-2
• 分子式：C₂₈H₃₆O₆
• 分子量：468.582
• 相关类别： 原料药 循环系统用药 调节血脂药
• 发布时间：2018-08-31 22:27:30
• 更新时间：2024-01-04 14:47:16
• Clinofibrate (S-8527)是一种降血脂药和一种HMG-CoA还原酶抑制剂。

名称

• 中文名: 克利贝特
• 英文名: Clinofibrate
• 英文别名: UNII:0374EZJ8CU; 2-[4-[1-[4-(2-carboxybutan-2-yloxy)phenyl]cyclohexyl]phenoxy]-2-methylbutanoic acid; 2,2'-[1,1-Cyclohexanediylbis(4,1-phenyleneoxy)]bis(2-methylbutanoic acid); 2,2'-[cyclohexane-1,1-diylbis(benzene-4,1-diyloxy)]bis(2-methylbutanoic acid); Butanoic acid, 2,2'-[cyclohexylidenebis(4,1-phenyleneoxy)]bis[2-methyl-; 2,2'-[Cyclohexane-1,1-diylbis(4,1-phenyleneoxy)]bis(2-methylbutanoic acid); MFCD00865769

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 613.8±55.0 °C at 760 mmHg
• 熔点: 143-145°C
• 分子式: C₂₈H₃₆O₆
• 分子量: 468.582
• 闪点: 198.1±25.0 °C
• 精确质量: 468.251190
• PSA: 93.06000
• LogP: 6.71
• 蒸汽压: 0.0±1.9 mmHg at 25°C
• 折射率: 1.559
• 储存条件: Refrigerator

生物活性

• 描述: Clinofibrate (S-8527)是一种降血脂药和一种HMG-CoA还原酶抑制剂。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> HMG-CoA还原酶(HMGCR)
  研究领域 >> 代谢疾病
• 体内研究: Clinofibrate给药(50和100 mg/kg /天,po)显着抑制血浆纤维蛋白原水平以及血清和VLDL-LDL-脂质的增加[1]。 Clinofibrate显着降低动脉粥样硬化大鼠的高血浆胆固醇水平,为823±256 mg/dl,或约为对照大鼠的10倍(85±11 mg/dl)。在使用clinofibrate治疗时,极低密度脂蛋白(VLDL)部分的胆固醇水平降低最多[2]。在禁食2天后再喂食无脂肪饮食或5％脂肪饮食的大鼠。 30 mg/kg的丙环酸酯可降低血清和肝脏甘油三酯水平[3]。将S-8527口服摄入正常大鼠7天后,血清甘油三酯和胆固醇分别在1mg/kg和2mg/kg时降低约27％。 3mg/kg的S-8527使肝脏甘油三酯浓度降低约20％[4]。
• 动物实验: 大鼠：使用体重100-160g的雄性Wistar大鼠。将S-8527和氯贝特悬浮在适量的阿拉伯树胶溶液中，使得每日剂量为每100g体重0.5mL。每天早上通过胃管将药物给予大鼠7天。对照组的车辆数量相等。在实验期间，动物随意喂食商业食物颗粒。在最后一次给药后约24小时，用乙醚麻醉大鼠，从下腔静脉获得血液样品。处死后，取出肝脏，用生理盐水洗涤，印在滤纸上并称重[4]。
• 参考文献:

  [1]. Okazaki M, et al. Effects of clinofibrate on plasma fibrinogen level in high fructose diet-induced hyperlipidemic rats. In Vivo. 1994 Nov-Dec;8(6):1057-61.

  [2]. Shirai K, et al. Effect of clinofibrate on lipid metabolism of aorta in atherosclerotic rats. Artery. 1983;12(3):145-55.

  [3]. Suzuki K, et al. Effects of S-8527 (1,1-bis4'-(1"-carboxy'1"-methylpropoxy)-phenyl)-cyclohexane), a new hypolipidemic compound, on triglyceride metablolism in rats. Biochem Pharmacol. 1975 Jun 15;24(11-12):1203-7.

  [4]. Suzuki K, et al. Hypolipidemic effect of a new aryloxy compound, S-8527, in experimental animals. Jpn J Pharmacol. 1974 Jun;24(3):407-14.

MSDS

Material Safety Data Sheet Section1. Identification of the substance Product Name: Clinofibrate 2-(4-{1-[4-(1-carboxy-1-methylpropoxy)phenyl]cyclohexyl}phenoxy)-2-methylbutanoic acid Synonyms: Section2. Hazards identification Harmful by inhalation, in contact with skin, and if swallowed. Section3. Composition/information on ingredients. Ingredient name:Clinofibrate CAS number:30299-08-2 Section4. First aid measures Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing contaminated clothing and shoes. If irritation persists, seek medical attention. Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical attention. Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention. Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention. Section5. Fire fighting measures In the event of a fire involving this material, alone or in combination with other materials, use dry powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus should be worn. Section6. Accidental release measures Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national standards. Respiratory precaution:Wear approved mask/respirator Hand precaution:Wear suitable gloves/gauntlets Skin protection:Wear suitable protective clothing Eye protection:Wear suitable eye protection Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container for disposal. See section 12. Environmental precautions: Do not allow material to enter drains or water courses. Section7. Handling and storage Handling:This product should be handled only by, or under the close supervision of, those properly qualified in the handling and use of potentially hazardous chemicals, who should take into account the fire, health and chemical hazard data given on this sheet. Store in closed vessels, refrigerated. Storage: Section8. Exposure Controls / Personal protection Engineering Controls: Use only in a chemical fume hood. Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles. General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse. Section9. Physical and chemical properties Appearance:Not specified Boiling point:No data No data Melting point: Flash point:No data Density:No data Molecular formula:C28H36O6 Molecular weight:468.6 Section10. Stability and reactivity Conditions to avoid: Heat, flames and sparks. Materials to avoid: Oxidizing agents. Possible hazardous combustion products: Carbon monoxide. Section11. Toxicological information No data. Section12. Ecological information No data. Section13. Disposal consideration Arrange disposal as special waste, by licensed disposal company, in consultation with local waste disposal authority, in accordance with national and regional regulations. Section14. Transportation information Non-harzardous for air and ground transportation. Section15. Regulatory information No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302, or have known CAS numbers that exceed the threshold reporting levels established by SARA Title III, Section 313. SECTION 16 - ADDITIONAL INFORMATION N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : ES8900000 CHEMICAL NAME : Butyric acid, 2,2'-cyclohexane-1,1-diylbis(p-phenyleneoxy)bis-(2-me thyl- CAS REGISTRY NUMBER : 30299-08-2 LAST UPDATED : 199612 DATA ITEMS CITED : 8 MOLECULAR FORMULA : C28-H36-O6 MOLECULAR WEIGHT : 468.64 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 : >4 gm/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: 6,219,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 205 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,933,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1930 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: 6,219,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >150 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: 6,219,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1600 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: 6,219,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 230 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair REFERENCE : YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 23,1553,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 350 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: 6,219,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 150 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,933,1981