CLINOFIBRATE (S-8527)
clinofibrate
CAS: 30299-08-2
Molecular Formula: C28H36O6
CLINOFIBRATE (S-8527) - Names and Identifiers
| Name | clinofibrate |
| Synonyms | lipoclin clinofibrate CLINOFIBRATE CLINOFIBRATE (S-8527) 1,1-Bis[4'-(1''-carboxy-1''-methylpropoxy)phenyl]cyclohexane 2,2'-(4,4'-cyclohexylidenediphenoxy)-2,2'-dimethyldibutyricacid 2,2'-cyclohexane-1,1-diylbis(p-phenyleneoxy)bis(2-methylbutyricacid) 2,2'-cyclohexane-1,1-diylbis(p-phenyleneoxy)bis-(2-methyl-butyricaci 2,2'-cyclohexane-1,1-diylbis(p-phenyleneoxy)bis(2-methylbutyricacid) 2,2'-(cyclohexylidenebis(4,1-phenyleneoxy))bis(2-methyl)-butanoic acid Butanoic acid, 2,2'-[cyclohexylidenebis(4,1-phenyleneoxy)]bis[2-methyl- 2,2'-[cyclohexane-1,1-diylbis(benzene-4,1-diyloxy)]bis(2-methylbutanoic acid) |
| CAS | 30299-08-2 |
| EINECS | 1312995-182-4 |
| InChI | InChI=1/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) |
CLINOFIBRATE (S-8527) - Physico-chemical Properties
| Molecular Formula | C28H36O6 |
| Molar Mass | 468.58 |
| Density | 1.1005 (rough estimate) |
| Melting Point | 143-145°C |
| Boling Point | 498.6°C (rough estimate) |
| Flash Point | 198.1°C |
| Solubility | Chloroform (Slightly), Methanol (Sligthly) |
| Vapor Presure | 6.38E-16mmHg at 25°C |
| Appearance | Solid |
| Color | White to Off-White |
| Merck | 14,2357 |
| pKa | 3.00±0.10(Predicted) |
| Storage Condition | Sealed in dry,Room Temperature |
| Refractive Index | 1.4482 (estimate) |
| In vitro study | Clinofrate is a lipid-lowering drug with an IC50 of 40 μm, which acts on the activity of human liver 3α-hydroxysteroid dehydrogenase. Clinofrate stimulated the activity of AKR 1C4 by 2 times. The maximum stimulation concentration of clinofrate was up to 50 μm. |
| In vivo study | Clinofrate significantly reduced high plasma cholesterol levels in atherosclerotic rats, 823 +/- 256 (mean +/- SD) mg/dl before clinofrate treatment, it was about 10 times that of control rats (85 +/- 11 mg/dl). Cholesterol levels in the very low density lipoprotein (VLDL) fraction (<1.006) decreased the most once clinofrated. Heparin-released lipoprotein lipase activity in epididymal adipose tissue, lipoprotein lipase activity in heparin plasma, and VLDL-triolein hydrolytic activity in interstitial vessels of adipose tissue in clinofrate-treated rats, than atherosclerotic rats. Enzymes in the arterial wall associated with cholesterol lipid metabolism and acid cholesteryl esterase activity were decreased in atherosclerotic rats, whereas clinoferrate treatment increased the activity. The ratio of acyl-coenzyme A cholesterol acyltransferase (ACAT) activity to Neutral cholesterol esterase activity was higher in atherosclerotic rats than in control rats, and lower in clinoferrate-treated rats than in atherosclerotic rats. Clinofrate is safe and effective in reducing VLDL in CAPD patients. A typical daily treatment at a dose of 600 mg resulted in a 36% reduction in serum triglycerides and a 48% reduction in VLDL triglycerides. Clinofrate also improved compositional abnormalities in the LDL and HDL components, and also significantly increased HDL cholesterol. |
CLINOFIBRATE (S-8527) - Risk and Safety
| RTECS | ES8900000 |
CLINOFIBRATE (S-8527) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.134 ml | 10.67 ml | 21.341 ml |
| 5 mM | 0.427 ml | 2.134 ml | 4.268 ml |
| 10 mM | 0.213 ml | 1.067 ml | 2.134 ml |
| 5 mM | 0.043 ml | 0.213 ml | 0.427 ml |
Last Update：2024-01-02 23:10:35
CLINOFIBRATE (S-8527) - Reference Information
| update date: | 2022/11/12 10:05:38 |
| Biological activity | Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR)(hydroxymethylglutaryl coenzyme A reductase),IC50 is 0.47 mM, is a lipid-lowering agent used to control high cholesterol and triglyceride levels in the blood. |
| Target | Value |
| HMGCR | 0.47 mM |
Last Update：2024-04-10 22:29:15
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