| CAS |
30299-08-2 |
| Chinese Name |
克利贝特 |
| English Name |
Clinofibrate |
| Synonyms |
S-8527;Lipoclin |
| Molecular Formula |
C28H36O6 |
| Molecular Weight |
468.58 |
| Solubility |
Soluble in DMSO ≥5mg/mL |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 1312995-182-4 |
| MDL |
MFCD00865769 |
| SMILES |
CCC(OC1=CC=C(C2(C3=CC=C(OC(CC)(C)C(O)=O)C=C3)CCCCC2)C=C1)(C)C(O)=O |
| InChIKey |
BMOVQUBVGICXQN-UHFFFAOYSA-N |
| InChI |
InChI=1S/C28H36O6/c1-5-26(3,24(29)30)33-22-14-10-20(11-15-22)28(18-8-7-9-19-28)21-12-16-23(17-13-21)34-27(4,6-2)25(31)32/h10-17H,5-9,18-19H2,1-4H3,(H,29,30)(H,31,32) |
| PubChem CID |
2787 |
| Target Point |
HMG-CoA Reductase (HMGCR) |
| Passage |
Metabolic Enzyme&Protease |
| Background |
Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) (hydroxymethylglutaryl coenzyme A reductase), a lipid-lowering agent used to control high cholesterol and triglyceride levels in the blood. |
| Biological Activity |
Clinofibrate (S-8527)是一种降血脂药和一种HMG-CoA还原酶抑制剂。[1-4] |
| In Vivo |
Clinofibrate给药(50和100 mg / kg /天，po)显著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显著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]。 |
| Animal Experiment |
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]。 |
| Data Literature Source |
[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. |
| Unit |
Bottle |
| Specification |
5mg 10mg 25mg |
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