Home
Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassay Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
Polymers & Contract Manufacturing
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Products
Small Molecule Inhibitors and Antagonist
Bioactive Compounds and Agonist
Primary Antibodies
Catalog Peptides
Amino Acids Derivatives
Reagents
Fluorescent dyes
Intermediates
PCR
Proteasomes and Enzymes
Enzyme substrate
Nucleotides
Promotions
Customer Support
About Us
Site Map
Contact Us
Small Molecule Inhibitors and Antagonist
Anti-virus
Cell Cycle
DMPK/Tox
Endocrinology
Epigenetics
GPCR/G-protein
Mitogen-activated Protein Kinases (MAPK)
PI3K/Akt/mTOR
Proteases/Proteasome
Protein Tyrosine Kinases (PTK)
Stem Cells
TGF-Beta/Smad
Transporter
Others
Cat. No. Name Size Price Add Cart
KI0985Gemfibrozil50 mg$154

Chemical Characteristic

Product NameGemfibrozil
SynonymsLopid
CAS No.25812-30-0
Molecular Weight 250.33
FormulaC15H22O3
Chemical Name5-?(2,?5-?dimethylphenoxy)?-?2,?2-?dimethyl-pentanoic acid
SmilesC(=O)(C(CCCOc1c(ccc(c1)C)C)(C)C)O
Chemical Structure

Biological activities

Gemfibrozil is a nonselective inhibitor of several P450 isoforms and uridine diphosphate glucuronosyltransferases. In vitro, gemfibrozil strongly inhibits CYP2C9, CYP2C19 and CYP1A2 with Ki of 5.8, 24 and 82 µM, respectively. Additionally, gemfibrozil inhibits paclitaxel 6a-hydroxylation with an IC50 of 91 µM. Gemfibrozil increases the risk of myopathy associated with simvastatin and lovastatin.[1] Gemfibrozil is an inhibitor of CYP- and UGT-mediated metabolism of cerivastatin (CER). Gemfibrozil significantly inhibits the OATP2-mediated uptake of CER and CYP2C8-mediated metabolism of CER with IC50 of 72 and 28 µM, respectively. Gemfibrozil inhibits CYP2C8-mediated M1 and M23 formation with IC50 of 36.8 and 29.7 µM, respectively. [2] Gemfibrozil lowers plasma PAI-118 in survivors of acute myocardial infarction. Gemfibrozil reduces basal PAI-1 synthesis by 20% and attenuates the TGF-β-induced 4.5-fold increase over 6 hours by 49%.[3]

Protocols

Gemfibrozil is dissolved in culture medium containing 0.1% DMF in final concentrations. [3]

References

[1] Wang JS, et al. Gemfibrozil inhibits CYP2C8-mediated cerivastatin metabolism in human liver microsomes. Drug Metab Dispos. 2002, 30(12): 1352-1356.
[2] Shitara Y, et al. Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1:SLC21A6)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil. J Pharmacol Exp Ther. 2004, 311(1): 228-236.
[3] Fujii S, et al. Direct effects of gemfibrozil on the fibrinolytic system. Diminution of synthesis of plasminogen activator inhibitor type 1. Circulation. 1992, 85(5): 1888-1893.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
About
KareBayTM Biochem
Sitemap
Blog
Custom Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Biochemical Products
Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR
Contact Us
KareBayTM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852
Telephone
: 732-823-1545

Fax
: 732-823-1349
product@karebaybio.com
service@karebaybio.com
support@karebaybio.com
Follow Us
Follow Karebay on LinkedinFollow IMAGING on Twitter Google+ Facebook