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Purity: ≥98%
Clinofibrate (Lipoclin; S-8527; S 8527) is a potent anti-hyperlipidemic agent which acts as an HMG-CoA (hydroxymethylglutaryl coenzyme A) reductase inhibitor with potential anti-hyperlipidemic effects. It inhibits HMG-CoA reductase (HMGCR) with an IC50 of 0.47 mM.
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Administration of clinofibrate at doses of 50 and 100 mg/kg/day, po, considerably reduces the rise in serum and VLDL-LDL-lipids as well as plasma fibrinogen levels[1]. The elevated plasma cholesterol level of atherosclerotic rats (823±256 mg/dl), which is almost ten times that of control rats (85±11 mg/dl), is dramatically reduced by clinofibrate. The very low density lipoprotein (VLDL) fraction experiences the greatest reduction in cholesterol levels when treated with clinofibrate[2]. After a two-day fast, rats are given a diet that is either fat-free or contains 5% fat. Serum and hepatic triglyceride levels are reduced when clinofibrate is administered at a dose of 30 mg/kg[3]. For seven days, normal rats given oral S-8527 reduce their serum cholesterol and triglycerides by approximately 20% at 3 mg/kg and 27% at 1 mg/kg, respectively. At 3 mg/kg, S-8527 reduces the level of liver triglycerides by approximately 20%[4].
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| 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 |
| Molecular Formula |
C28H36O6
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| Molecular Weight |
468.58
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| CAS # |
30299-08-2
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| SMILES |
CCC(C)(OC1=CC=C(C2(C3=CC=C(OC(CC)(C(O)=O)C)C=C3)CCCCC2)C=C1)C(O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.34 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.34 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1341 mL | 10.6705 mL | 21.3411 mL | |
| 5 mM | 0.4268 mL | 2.1341 mL | 4.2682 mL | |
| 10 mM | 0.2134 mL | 1.0671 mL | 2.1341 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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