| Bioactivity | 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]. | |||||||||
| Invitro | Gemfibrozil 1-O-β-Glucuronide significantly inhibits the OATP2 (OATP1B1)-mediated uptake of Cerivastatin (CER; HY-129458) with an IC50 of 24.3 μM[1]. 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[1]. Gemfibrozil 1-O-β-Glucuronide has an IC50 of 243 μM for the CYP3A4- mediated metabolism[1]. | |||||||||
| Name | Gemfibrozil 1-O-β-glucuronide | |||||||||
| CAS | 91683-38-4 | |||||||||
| Formula | C21H30O9 | |||||||||
| Molar Mass | 426.46 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. |
Gemfibrozil 1-O-β-glucuronide
CAS: 91683-38-4 F: C21H30O9 W: 426.46
Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) i
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