CAS 30299-08-2|Clinofibrate
| Common Name | Clinofibrate | ||
|---|---|---|---|
| CAS Number | 30299-08-2 | Molecular Weight | 468.582 |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 613.8±55.0 °C at 760 mmHg |
| Molecular Formula | C28H36O6 | Melting Point | 143-145°C |
| MSDS | / | Flash Point | 198.1±25.0 °C |
Names
| Name | Clinofibrate |
|---|---|
| Synonym | More Synonyms |
Clinofibrate BiologicalActivity
| Description | Clinofibrate (S-8527) is a hypelipidemic agent and a HMG-CoA reductase inhibitor. |
|---|---|
| Related Catalog | Signaling Pathways >>Metabolic Enzyme/Protease >>HMG-CoA Reductase (HMGCR)Research Areas >>Metabolic Disease |
| In Vivo | Clinofibrate administration (50 and 100 mg/kg/day, p.o.) significantly inhibits the increase in plasma fibrinogen level as well as serum- and VLDL-LDL-lipids[1]. Clinofibrate significantly decreases the high plasma cholesterol level of atherosclerotic rats, which is 823±256 mg/dl, or about ten times that of control rats (85±11 mg/dl). On treatment with clinofibrate, the cholesterol level is reduced most in the very low density lipoprotein (VLDL) fraction[2]. In rats which are refed either a fat-free diet or a 5% fat diet after a 2-day fast. clinofibrate at 30 mg/kg results in reductions of serum and liver triglyceride levels[3]. Oral ingestion of S-8527 to normal rats for 7 days lowers serum triglycerides and cholesterol by about 27% at 1 mg/kg and 20% at 3 mg/kg, respectively. S-8527 at 3 mg/kg decreases liver triglyceride concentration by about 20%[4]. |
| Animal Admin | Rats: Male Wistar rats weighing 100-160 g are used. S-8527 and clofibrate are suspended in an appropriate amount of 5 gum arabic solution so that the daily dose would be 0.5 mL per 100 g of body weight. The drugs are given to the rats via stomach tube every a.m. for 7 days. Control groups are on an equal volume of vehicle. During the experimental period, the animals are fed on a commercial chow pellet ad libitum. About 24 hr after the last dose, the rats are anesthetized with ether and blood samples are obtained from the inferior venacava. After sacrifice, the livers are removed, washed with physiological saline, blotted on filter paper and weighed[4]. |
| References | [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. |
Chemical & Physical Properties
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 613.8±55.0 °C at 760 mmHg |
| Melting Point | 143-145°C |
| Molecular Formula | C28H36O6 |
| Molecular Weight | 468.582 |
| Flash Point | 198.1±25.0 °C |
| Exact Mass | 468.251190 |
| PSA | 93.06000 |
| LogP | 6.71 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.559 |
| InChIKey | BMOVQUBVGICXQN-UHFFFAOYSA-N |
| SMILES | CCC(C)(Oc1ccc(C2(c3ccc(OC(C)(CC)C(=O)O)cc3)CCCCC2)cc1)C(=O)O |
| Storage condition | Refrigerator |
Toxicological Information
CHEMICAL IDENTIFICATION |
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
Synonyms
| 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 |
