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Clinofibrate

Cat. No. M3527
Clinofibrate Structure
Synonym:

S-8527

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 75  USD75 In stock
50mg USD 300  USD300 In stock
100mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

Clinofibrate is a new hypelipidemic agent and a competitive hydroxymethylglutaryl coenzyme A reductase with an IC50 of 0.47 mM. Clinofibrate is a derivative of clofibrate. Clinofibrate, as a antihyperlipidemic drug, activiates human liver 3alpha-hydroxysteroid dehydrogenase. The optimal pha of activation this enzyme by the compound clinofibrate was about 7.5. The concentrations giving maximum stimulation (1.8 to 2.4 fold) for clinofibrate were 50 μM. The activation by the antihyperlipidemic drug, clinofibrate, elevated both Km and Kcat (turnover number) values for the coenzyme and substrates. Clinofibrate lacks the chloro group, methyl goup on the alpha-carbon or carboxyl group. Thus, clinofibrate greatly decreased the stimulatory effects. Kinetic analysis with respect to NAPD+ exhibited that clinofibrate was nonessential activators with dissociation constants of 6 μM. These data suggest that the long-term treatment with the antihyperlipidemic drugs generates effects on the metabolism of steroid hormones and bile acids, as well as several-containing drugs mediated by the enzyme.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Seven-week-old Sprague-Dawley rats (SLC), six-week-old ICR-SLC mice and a one-year-old beagle dog
Formulation
Dosages 30 mg/kg
Administration Administered orally or intravenously
Chemical Information
Molecular Weight 468.58
Formula C28H36O6
CAS Number 30299-08-2
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yohtaro Sato, et al. Clinofibrate improved canine lipid metabolism in some but not all breeds

[2] Jian-kang Li, et al. Effect of food on the single-dose pharmacokinetics and tolerability of clinofibrate tablets in Chinese healthy volunteers

[3] Li Jian-Kang, et al. High-performance liquid chromatographic method for determination of clinofibrate and its application to a pharmacokinetic study in healthy volunteers

[4] N Takeuchi, et al. Effect of clinofibrate, a new hypolipidemic agent, on biliary and serum lipids in patients with hyperlipidemia

[5] S Okada, et al. Clinofibrate therapy raises high-density lipoprotein levels and lowers atherogenic index in diabetes mellitus patients

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Keywords: Clinofibrate, S-8527 supplier, HMG-CoA Reductase, inhibitors, activators


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