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Chemical Structure| 25812-30-0 Chemical Structure| 25812-30-0

Structure of Gemfibrozil
CAS No.: 25812-30-0

Chemical Structure| 25812-30-0

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Gemfibrozil is an agonist of PPARα. It can act as a hyperlipidemic agent that elevates plasma HDL and lowers triglycerides.

Synonyms: CI-719

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Product Details of Gemfibrozil

CAS No. :25812-30-0
Formula : C15H22O3
M.W : 250.33
SMILES Code : O=C(C(C)(CCCOC1=C(C)C=CC(C)=C1)C)O
Synonyms :
CI-719
MDL No. :MFCD00079335
InChI Key :HEMJJKBWTPKOJG-UHFFFAOYSA-N
Pubchem ID :3463

Safety of Gemfibrozil

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H351-H413
Precautionary Statements:P501-P273-P270-P264-P301+P312+P330-P202

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse primary astrocytes 10 μM 24 hours GFB-RA treatment enhanced the uptake of Aβ in astrocytes via LDLR-mediated endocytosis. Sci Signal. 2021 Oct 26;14(706):eabg4747
hippocampal neurons 25 μM 24 hours Gemfibrozil significantly induced ADAM10 expression and reduced Aβ production Proc Natl Acad Sci U S A. 2015 Jul 7;112(27):8445-50
Beas2b cells 10 μM 12 hours Gemfibrozil significantly reduces CSE-induced autophagy impairment and aggresome formation by inducing TFEB and controlling ROS activity. Antioxid Redox Signal. 2017 Jul 20;27(3):150-167
human microglia (HM) cells different concentrations 24 hours Gemfibrozil increased the protein level of LC3B-II:LC3B-I and decreased the protein level of SQSTM1 in a dose-dependent manner, indicating autophagy induction. Autophagy. 2020 Jan;16(1):52-69
Acinetobacter baylyi ADP1 0.005, 0.05, 0.5, 5, 50 mg/L 6 hours To investigate the effect of gemfibrozil on the transformation frequency of Acinetobacter baylyi ADP1. Results showed that gemfibrozil significantly increased the transformation frequency of ARGs at concentrations as low as 0.005 mg/L, reaching up to 5.97 × 10−6 per total bacteria. ISME J. 2020 Aug;14(8):2179-2196
COS7 cells 100 μM To evaluate the response of α1C517Yβ1 sGC variant to gemfibrozil, results showed that α1C517Yβ1 sGC had a stronger response to gemfibrozil compared to wild-type sGC Biochem Pharmacol. 2021 Apr;186:114459
U251-APP cells 200 μM 24 hours Gemfibrozil treatment increased LC3B-II:LC3B-I protein levels and decreased SQSTM1 protein levels, indicating autophagy induction. Autophagy. 2020 Jan;16(1):52-69

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice 5XFAD mouse model Oral 8 mg/kg/day GFB + 150 IU/day RA Once daily for 60 days Oral GFB-RA stimulated lysosomal biogenesis, reduced plaque load and improved spatial learning and memory in the 5XFAD mouse model of AD via astroglial PPAR α. Sci Signal. 2021 Oct 26;14(706):eabg4747
Mice APP-PSEN1 ΔE9 mouse model Oral administration in drinking water 50 μg/mL For 2 months Gemfibrozil improved spatial learning and memory deficits, reduced anxiety symptoms, and decreased soluble and insoluble Aβ levels in the hippocampus and cortex tissues of APP-PSEN1 ΔE9 mice. Autophagy. 2020 Jan;16(1):52-69
Wistar rats Male Wistar rats Transdermal administration 46 mg/kg (transdermal administration) 24 hours To investigate the pharmacokinetic properties of Gemfibrozil in transdermal drug delivery system Acta Pharm Sin B. 2020 May;10(5):928-945
C57BL/6 mice Subchronic cigarette smoke-induced COPD-emphysema model Intraperitoneal injection 40 mg/kg body weight Alternate days for 10 days Gemfibrozil significantly reduces CS-induced autophagy impairment, inflammation (IL-6 levels), apoptosis (caspase-3/7 activity), and emphysema (alveolar airspace enlargement) by inducing TFEB. Antioxid Redox Signal. 2017 Jul 20;27(3):150-167

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00108511 Hypertriglyceridemia PHASE1 COMPLETED 2025-09-07 Roudebush VA Medical Center, I... More >>ndianapolis, Indiana, 46202, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.99mL

0.80mL

0.40mL

19.97mL

3.99mL

2.00mL

39.95mL

7.99mL

3.99mL

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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