Gemfibrozil 1-O-β-glucuronide

Gemfibrozil 1-O-β-glucuronide

• CAS Number: 91683-38-4
• UNSPSC Description: 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].
• Target Antigen: Cytochrome P450; Drug Metabolite; PPAR
• Type: Reference compound
• Related Pathways: Cell Cycle/DNA Damage;Metabolic Enzyme/Protease;Vitamin D Related/Nuclear Receptor
• Field of Research: Metabolic Disease; Cardiovascular Disease
• Assay Protocol: https://www.medchemexpress.com/gemfibrozil-1-o-β-glucuronide.html
• 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 Weight: 426.46
• 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.
• Shipping Conditions: Blue Ice
• Storage Conditions: -20°C, 3 years (Powder)
• Clinical Information: No Development Reported