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Gemfibrozil 1-O-β-glucuronide

Catalog No. T11387 CAS 91683-38-4

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 μM.

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Gemfibrozil 1-O-β-glucuronide Chemical Structure

Gemfibrozil 1-O-β-glucuronide, CAS 91683-38-4

Pack Size	Availability	Price/USD	Quantity
500 μg	4-5 weeks	$ 592.00
1 mg	4-5 weeks	$ 1,140.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	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 μM.
Targets&IC50	CYP2C8:4.07 μM
In vitro	Gemfibrozil 1-O-β-Glucuronide inhibits CYP2C8-mediated M1, M23 formation with IC50s of 5.38 μM, 4.30 μM, and has no effects for CYP2C8-mediated M3 formation.??Gemfibrozil 1-O-β-Glucuronide has an IC50 of 243 μM for the CYP3A4- mediated metabolism.Gemfibrozil 1-O-β-Glucuronide significantly inhibits the OATP2 (OATP1B1)-mediated uptake of Cerivastatin with an IC50 of 24.3 μM.

Molecular Weight	426.46
Formula	C21H30O9
CAS No.	91683-38-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

Gemfibrozil 1-O-β-glucuronide 91683-38-4 Others Gemfibrozil 1-O-beta-glucuronide Gemfibrozil 1Oβglucuronide Gemfibrozil 1-O-b-glucuronide Gemfibrozil 1 O β glucuronide inhibitor inhibit

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