Home Metabolism HMG-CoA Reductase inhibitor Clinofibrate For research use only.

Clinofibrate

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.

Clinofibrate Chemical Structure

Clinofibrate Chemical Structure

CAS No. 30299-08-2

Purity & Quality Control

Clinofibrate Related Products

Signaling Pathway

HMG-CoA Reductase Signaling Pathways

HMG-CoA Reductase Signaling Pathway

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.
Targets
HMGCR [1]
0.47 mM
In vitro
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]
In Vivo
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]

Chemical Information & Solubility

Molecular Weight 468.58 Formula

C28H36O6
CAS No. 30299-08-2 SDF Download Clinofibrate SDF
Smiles CCC(C)(C(=O)O)OC1=CC=C(C=C1)C2(CCCCC2)C3=CC=C(C=C3)OC(C)(CC)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (200.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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