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Chemical Structure| 637-07-0 Chemical Structure| 637-07-0

Structure of Clofibrate
CAS No.: 637-07-0

Chemical Structure| 637-07-0

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Clofibrate, a fibric acid derivative, is a selective agonist of peroxisome proliferator-activated receptor α (PPARα) with EC50 of 50 µM. Clofibrate has been used to treat hyperlipoproteinemia type III and severe hypertriglyceridemia.

Synonyms: ICI 28257; NSC 79389; Clofibratum

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Product Details of Clofibrate

CAS No. :637-07-0
Formula : C12H15ClO3
M.W : 242.70
SMILES Code : CC(C)(OC1=CC=C(Cl)C=C1)C(OCC)=O
Synonyms :
ICI 28257; NSC 79389; Clofibratum
MDL No. :MFCD00000615
InChI Key :KNHUKKLJHYUCFP-UHFFFAOYSA-N
Pubchem ID :2796

Safety of Clofibrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335-H351-H361
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 500 μM 48 h Clofibrate promoted PPAR-α expression and decreased miR-17-5p levels, inhibiting steatosis Mol Ther. 2015 Jul;23(7):1222-1233

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Newborn pigs Newborn pig model Oral gavage 75 mg/kg body weight Once daily for 4 days Evaluate the effect of PPARα activation on fatty acid oxidation in the kidneys of newborn pigs, showing a significant increase in mitochondrial fatty acid oxidation. Int J Mol Sci. 2017 Dec 8;18(12):2663
Sprague Dawley rats 5/6 nephrectomy model Intraperitoneal injection 25 mg/kg Once daily for 5 weeks To test the therapeutic effect of the PPARα agonist clofibrate on cardiac function in 5/6Nx rats. Clofibrate treatment improved cardiac function, reduced LV dilation, and increased ejection fraction. Kidney Int. 2018 Feb;93(2):375-389
Rat Spontaneously hypertensive rats (SHR) Intraperitoneal injection 250 mg/kg Once daily for 21 days To examine the effects of clofibrate on blood pressure and vascular reactivity in spontaneously hypertensive rats (SHR). Results showed that clofibrate significantly reduced systolic blood pressure (26%±2%) and proteinuria (43%±9%) in SHR, increased urinary nitrite/nitrate excretion, enhanced PPARα protein expression and activity, and attenuated the vasoconstrictor response of aortic rings. Acta Pharmacol Sin. 2014 Apr;35(4):476-82
Rats and squirrel monkeys Nicotine self-administration model Intraperitoneal (rats), intramuscular (monkeys) 100-300 mg/kg (rats), 25-100 mg/kg (monkeys) Once daily, lasting from several days to weeks Clofibrate prevented the rewarding effects of nicotine in naive animals, substantially decreased nicotine intake in experienced animals, and counteracted the relapse-inducing effects of re-exposure to nicotine or nicotine-associated cues after a period of abstinence. Additionally, clofibrate blocked nicotine’s effects on neuronal firing in the ventral tegmental area and dopamine release in the nucleus accumbens shell. Neuropsychopharmacology. 2012 Jul;37(8):1838-47
Sprague-Dawley rats KS-type and NC-type GST M1 gene polymorphic rats Oral 0.3% w/w 4 weeks To investigate the effects of Clofibrate on the induction of bifunctional enzyme (BE) in rat livers and its relation to hepatocarcinogenesis. Results showed that KS-type rats exhibited higher BE induction and preneoplastic hepatic foci after CF treatment. Cancer Sci. 2010 Apr;101(4):869-75
Mice Methionine-choline-deficient (MCD) diet-induced fatty liver model Oral 0.5% (w/w) Continuous for 14 days To evaluate the effect of Clofibrate on MCD diet-induced hepatic stress signaling. Results showed that Clofibrate eliminated MCD-mediated hepatic steatosis but did not inhibit diet-induced stress. Gastroenterology. 2010 Nov;139(5):1730-9, 1739. e1
Mice PPARα-null (Ppara−/−) mice and wild-type (Ppara+/+) mice Dietary administration 1.0% (w/w) 7 days Inhibiting spontaneous down-regulation of PPARα post-transplantation, by enhancing the expression and activity of fatty acid oxidation enzymes, increased oxidative stress and hepatocellular injury. J Hepatol. 2012 Mar;56(3):586-94

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03031821 Prostate Cancer ... More >> Metabolic Syndrome Less << Phase 3 Not yet recruiting June 1, 2023 Canada, British Columbia ... More >> BC Cancer Agency - Vancouver Cancer Centre Not yet recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Bernie Eigl, MD    604-877-6000    bernie.eigl@bccancer.bc.ca    Principal Investigator: Bernie Eigl, MD Less <<
NCT00000483 Cardiovascular Diseases ... More >> Coronary Disease Heart Diseases Myocardial Infarction Myocardial Ischemia Less << Not Applicable Completed - -
NCT00000482 Cardiovascular Diseases ... More >> Coronary Disease Heart Diseases Myocardial Infarction Myocardial Ischemia Less << Phase 3 Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.12mL

0.82mL

0.41mL

20.60mL

4.12mL

2.06mL

41.20mL

8.24mL

4.12mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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