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Clinofibrate

Cat. No. M3527
Clinofibrate Structure
Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 240 In stock
200mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 468.58
Formula C28H36O6
CAS Number 30299-08-2
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Clinofibrate supplier, HMG-CoA Reductase, inhibitors

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