Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil, is a potent and competitive inhibitor of P450 (CYP) isoform CYP2C8, with an IC50 of 4.07 μM.
Ifenprodil glucuronide, a derivative of Ifenprodil, is a vasodilator and an inhibitor of platelet aggregation. In contrast to Ifenprodil, Ifenprodil glucuronide does not affect platelet aggregation nor arterial contraction.
Raloxifene 6,4'-Bis-β-D-glucuronide, a metabolite of Raloxifene, acts as a selective antagonist of the estrogen receptor used for osteoporosis prevention.
MAC glucuronide phenol-linked SN-38, a pH-sensitive lactone and DNA topoisomerase I inhibitor drug linker, exhibits cytotoxicity in L540cy and Ramos cells, with IC50 values of 113 ng mL and 67 ng mL, respectively[1].
MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells
Darexaban glucuronide is the major component in plasma after oral administration of darexaban to humans. Darexaban (YM150) is a direct inhibitor of factor Xa.
(±)-4-hydroxy Propranolol β-D-glucuronide is a metabolite of (±)-4-hydroxy propranolol , which is a metabolite of propranolol. The apparent half-life of (±)-4-hydroxy propranolol β-D-glucuronide is similar to propranolol and 4-hydroxy propranolol. Propranolol is a β-adrenergic antagonist, and the active enantiomer, (S)-(-)-propranolol , has log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively.