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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEClinofibrateCat. No.: HY-13528CAS No.: 30299-08-2Synonyms: S-8527分式: CHO分量: 468.58作靶点: HMG-CoA Reductase (HMGCR)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO :

2、 30 mg/mL (64.02 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1341 mL 10.6705 mL 21.3411 mL5 mM 0.4268 mL 2.1341 mL 4.2682 mL10 mM 0.2134 mL 1.0671 mL 2.1341 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Clinofibrate (S-8527)种

3、降脂药和种HMG-CoA还原酶抑制剂。体内研究Clinofibrate administration (50 and 100 mg/kg/day, p.o.) significantly inhibits the increase in plasmafibrinogen level as well as serum- and VLDL-LDL-lipids 1. Clinofibrate significantly decreases the highplasma cholesterol level of atherosclerotic rats, which is 823256 mg/dl,

4、 or about ten times that of control rats1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE(8511 mg/dl). On treatment with clinofibrate, the cholesterol level is reduced most in the very low densitylipoprotein (VLDL) fraction 2. In rats which are refed either a fat-free diet or a 5% fat diet after a 2

5、-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 con

6、centration by about 20% 4.PROTOCOLAnimal Rats: Male Wistar rats weighing 100-160 g are used. S-8527 and clofibrate are suspended in an appropriateAdministration 4 amount of 5 gum arabic solution so that the daily dose would be 0.5 mL per 100 g of body weight. The drugsare given to the rats via stoma

7、ch tube every a.m. for 7 days. Control groups are on an equal volume ofvehicle. During the experimental period, the animals are fed on a commercial chow pellet ad libitum. About24 hr after the last dose, the rats are anesthetized with ether and blood samples are obtained from theinferior venacava. A

8、fter sacrifice, the livers are removed, washed with physiological saline, blotted on filterpaper and weighed 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Okazaki M, et al. Effects of clinofibrate on plasma fibrinogen level in high fruc

9、tose 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-carboxy1-methylpropoxy)-phenyl)-cyclohexane), a new

10、hypolipidemic compound, ontriglyceride 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. 1974Jun;24(3):407-14.McePdfHeightCaution: Product has not been fully validat

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