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克利贝特

克利贝特用途

Clinofibrate (S-8527)是一种降血脂药和一种HMG-CoA还原酶抑制剂。

克利贝特名称

[ CAS 号 ]:
30299-08-2

[ 中文名 ]:
克利贝特

[ 英文名 ]:
Clinofibrate

[英文别名 ]:

UNII:0374EZJ8CU
MFCD00865769

克利贝特生物活性

[ 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.

[相关活性小分子]

克利贝特物理化学性质

[ 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

克利贝特MSDS

详细MSDS(安全技术说明书)

克利贝特毒性和生态

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