Activity of human UGT1A10 expressed in microsomes isolated from baculovirus infected insect cell assessed as enzyme-mediated (2S,3S,4S,5R,6R)-3,4,5-trihydroxy-6-(5-(4-((6-methoxy-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzyl)-2,4-dioxothiazolidin-3-yl)tetrahydro-2H-pyran-2-carboxylic acid formation at 20 uM after 4 hrs by radio-HPLC/LC-MS/MS analysis in presence of UDPGA
Drug metabolism assessed as human recombinant UGT1A10-mediated (2S,3S,4S,5R,6S)-6-(2-(4-(4-(tert-butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid formation at 10 uM after 30 mins by LC-MS/MS analysis
Drug metabolism assessed as human UGT1A10-mediated 13-epiestradiol-3-glucuronide formation at 200 uM after 15 to 60 mins by HPLC analysis in presence of UDPGA
Drug metabolism assessed as recombinant human C-terminal His-tagged UGT1A10-mediated 17-epiestriol-3-glucuronide formation at 200 uM after 15 to 60 mins by HPLC analysis in presence of UDPGA
Drug metabolism assessed as recombinant human C-terminal His-tagged UGT1A10-mediated 17-epiestriol-3-glucuronide formation after 15 to 60 mins by Michaelis-Menten equation analysis in presence of UDPGA
Drug metabolism in human KB3 cells overexpressing human UGT1A10 assessed as enzyme-mediated metabolites formation at 30 uM for 24 to 72 hrs by HPLC analysis and electrospray ionization-mass spectrometry
Drug metabolism assessed as human UGT1A10-mediated N-glucuronide-triclocarban formation expressed in baculovirus infected insect sf9 cells incubated for 5 mins prior to UDPGA addition measured after 5 to 30 mins by LC-UV analysis
Drug metabolism in human KB3 cells overexpressing human UGT1A10 assessed as enzyme-mediated metabolites formation at 30 uM for 24 to 72 hrs by HPLC analysis
Drug metabolism assessed as human UGT1A10-mediated N'-glucuronide-triclocarban formation expressed in baculovirus infected insect sf9 cells incubated for 5 mins prior to UDPGA addition measured after 5 to 30 mins by LC-UV analysis
Activity of recombinant human UGT1A10 expressed in baculovirus-infected insect cells assessed as enzyme-mediated glucuronidation per mg of protein after 10 mins in presence of UDPGA
Drug level assessed as recombinant human C-terminal His-tagged UGT1A10-mediated compound formation from 200 uM 16-epiestriol after 15 to 60 mins by Michaelis-Menten equation analysis in presence of UDPGA