Gemfibrozil 1-O-β-glucuronide-d6

Gemfibrozil 1-O-β-glucuronide-d6 is the deuterium labeled Gemfibrozil 1-O-β-glucuronide (HY-129993) . Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM[1][2].

Product Specifications

CAS Number

[1703747-47-0]

UNSPSC

12352005

Target

Cytochrome P450; Drug Metabolite; Isotope-Labeled Compounds; PPAR

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease; Others; Vitamin D Related/Nuclear Receptor

Field of Research

Metabolic Disease

Smiles

CC(C=CC(C)=C1)=C1OCCCC(C([2H])([2H])[2H])(C([2H])([2H])[2H])C(O[C@@H]2O[C@@H]([C@H]([C@@H]([C@H]2O)O)O)C(O)=O)=O

Molecular Formula

C21H24D6O9

Molecular Weight

432.49

References & Citations

[1]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.|[2]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.