Clinofibrate
For research use only.
Catalog No.S2664
1 publication
CAS No. 30299-08-2
Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM, is a lipid-lowering agent used for controlling high cholesterol and triacylglyceride levels in the blood.
Selleck's Clinofibrate has been cited by 1 publication
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Choose Selective HMG-CoA Reductase Inhibitors
Biological Activity
| Description | Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM, is a lipid-lowering agent used for controlling high cholesterol and triacylglyceride levels in the blood. | ||
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| Targets |
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| In vitro |
Clinofibrate is an antihyperlipidemic agent with IC50 with 40 μM on the activities of human liver 3α-hydroxysteroid dehydrogenases. Clinofibrate stimulates the activity of AKR 1C4 by 2.0-fold. The concentration of Clinofibrate at which maximum stimulation is achieved is 50 μM. [1] |
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| In vivo | Clinofibrate significantly decreases the high plasma cholesterol level of atherosclerotic rats, which is 823 +/- 256 (mean +/- SD) mg/dl, or about ten times that of control rats (85 +/- 11 mg/dl). On treatment with Clinofibrate, the cholesterol level is reduced mostly in the very low density lipoprotein (VLDL) fraction (d less than 1.006). Heparin-releasable lipoprotein lipase activity in epididymal adipose tissue, lipoprotein lipase activity in post heparin plasma, and VLDL-triolein hydrolizing activity in adipose tissue stromal vessels are higher in Clinofibrate-treated rats than in atherosclerotic rats. Of the enzymes in the arterial wall concerned with cholesterol ester metabolism, acid cholesterol esterase activity is decreased in atherosclerotic rats, and Clinofibrate treatment increased this activity. The ratio of acyl-CoA cholesterol acyltransferase activity (ACAT) to neutral cholesterol esterase activity is higher in atherosclerotic rats than in control rats and is lower in Clinofibrate-treated rats than in atherosclerotic rats. [2] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 94 mg/mL (200.6 mM) |
|---|---|---|
| Ethanol | 94 mg/mL (200.6 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 468.58 |
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| Formula | C28H36O6 |
| CAS No. | 30299-08-2 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | CCC(C)(C(=O)O)OC1=CC=C(C=C1)C2(CCCCC2)C3=CC=C(C=C3)OC(C)(CC)C(=O)O |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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