Gemfibrozil 1-O-β-glucuronide

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

[91683-38-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Cytochrome P450; Drug Metabolite; PPAR

Type

Reference compound

Related Pathways

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

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/gemfibrozil-1-o-β-glucuronide.html

Concentration

10mM

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O[C@H]1[C@H](OC(C(C)(C)CCCOC2=CC(C)=CC=C2C)=O)O[C@H](C(O)=O)[C@@H](O)[C@@H]1O

Molecular Formula

C21H30O9

Molecular Weight

426.46

Precautions

H302, H315, H319, H335

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.