TargetMol

Gemfibrozil 1-O-β-glucuronide

Product Code:
 
TAR-T11387
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil , is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 uM.
CAS:
91683-38-4
Formula:
C21H30O9
Molecular Weight:
426.46
Purity:
0.98
SMILES:
O(C(C(CCCOC1=C(C)C=CC(C)=C1)(C)C)=O)[C@@H]2O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]2O

References

Baer BR, et al. Benzylic oxidation of gemfibrozil-1-O-beta-glucuronide by P450 2C8 leads to heme alkylation and irreversible inhibition. Chem Res Toxicol. 2009 Jul;22(7):1298-309. 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 Oct;311(1):228-36.