Drug metabolism assessed as UGT1A4-mediated compound glucuronidation in pooled mixed-gender human liver microsomes at 50 uM preincubated at 37 degC for 3 mins before UDPGA addition by HPLC method
Drug metabolism assessed as UGT1A4 activity in human liver microsome assessed as of N-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis
Drug metabolism assessed as recombinant human UGT1A4 assessed as O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis in presence of 10 uM hecogenin relative to control
Activity of human UGT1A4 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 recombinant human UGT1A4 assessed as O-glucuronidation measured per mg of protein at 10 to 400 uM incubated for 60 mins by LC-MS/MS analysis
Drug metabolism assessed as UDPGA-fortified human recombinant UGT1A4-mediated DTG glucuronide metabolite ((2S,3S,4S,5R,6S)-6-((4R,12aS)-9-(2,4-difluorobenzylcarbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazin-7-yloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid) formation at 16 uM after 120 mins by radio-HPLC analysis
Drug metabolism assessed as recombinant human C-terminal His-tagged UGT1A4-mediated 17-epiestriol-16-glucuronide formation at 200 uM after 15 to 60 mins by HPLC analysis in presence of UDPGA