8-Hydroxywarfarin

8-Hydroxywarfarin (750 μM; 90 min) is glucuronidated by recombinant wild-type UGT1A10 and its UGT1A10^F90A, UGT1A10^F93A, and UGT1A10^V92A mutants expressed in baculovirus-infected Sf9 insect cells at specific activities of 20, 20, 50, and 183 nmol/min/mg protein, respectively^[1].
8-Hydroxywarfarin (100-2000 μM; 90 min) is glucuronidated via Michaelis-Menten kinetics by recombinant wild-type UGT1A10 and its UGT1A10^F90A, UGT1A10^V92A, and UGT1A10^F93A mutants expressed in baculovirus-infected Sf9 insect cells, with V_max values of 25, 18, 260, and 69 nmol/min/mg protein and K_m values of 390, 190, 390, and 304 μM, respectively^[1].
8-Hydroxywarfarin (250 μM; 90 min) glucuronidation by recombinant wild-type UGT1A10 and its F90A, V92A, and F93A mutants expressed in baculovirus-infected Sf9 insect cells is competitively inhibited by Warfarin, 6-hydroxywarfarin, and 7-hydroxywarfarin, with K_i values ranging from 300 μM to ≥1500 μM depending on the inhibitor and enzyme variant^[1].
8-Hydroxywarfarin (750 μM; 180 min) is metabolized to an identical 8-O-glucuronide metabolite by recombinant wild-type UGT1A10 and its UGT1A10^F90A, UGT1A10^V92A, and UGT1A10^F93A mutants expressed in baculovirus-infected Sf9 insect cells, as confirmed by LC-MS/MS analysis^[1].
8-Hydroxywarfarin (750 μM; up to 180 min) is catalyzed for glucuronidation in vitro by UGT1A1, UGT1A3, UGT1A8, UGT1A9, and UGT1A10, with UGT1A10 exhibiting the highest activity (>0.6 μM/mg protein/min) at a substrate concentration of 750 μM^[2].
8-Hydroxywarfarin (100-2000 μM; 90 min) is catalyzed for glucuronidation in vitro by UGT1A8, UGT1A9, and UGT1A10 with defined Michaelis-Menten kinetic parameters, where UGT1A10 exhibits the highest catalytic efficiency (V_max/K_m = 2.3 ×10^-3 min^-1 mg^-1 protein)^[2].
8-Hydroxywarfarin is glucuronidated by human UGTs in vitro, forming a conjugate confirmed via LC-MS/MS with characteristic mass spectral fragments^[2].
8-Hydroxywarfarin (100 μM; 60 min) significantly inhibits recombinant human CYP2C9-mediated 6-hydroxylation of (S)-warfarin in vitro by approximately 85%^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.