Prodrug conversion in Homo sapiens (human) liver cytosol assessed as (S)-3-(1-(benzo[d][1,3]dioxol-5-yl)-2-(2-methoxy-4-methylphenylsulfonamido)-2-oxoethyl)-1-methyl-1H-indole-6-carboxylic acid formation
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation in presence of pargyline by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation in presence of allopurinol by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation after 60 mins by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation per mg protein after 60 mins by LC-MS/MS/FSA method
Ratio of Vmax to Km for drug metabolism in human liver cytosol assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation per mg protein after 60 mins by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation after 60 mins by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation per mg protein after 60 mins by LC-MS/MS/FSA method
Ratio of Vmax to Km for drug metabolism in human liver cytosol assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation per mg protein after 60 mins by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation at 20 uM after 60 mins in presence of co-incubation with ritonavir by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2S,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation at 20 uM after 60 mins in presence of pre-incubation with ritonavir by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation in presence of flufenamic acid by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation at 20 uM after 60 mins in presence of AKR inhibitor diazepam by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation at 20 uM after 60 mins in presence of AKR inhibitor ibuprofen by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol at 20 uM assessed as (1R,2S,5S)-N-((2R,3R)-4-amino-1-cyclobutyl-3-hydroxy-4-oxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide formation in presence of BNPP by LC-MS/MS/FSA method
Drug metabolism in human liver cytosol treated with 20 uM [14C]SCH 534129 assessed as 100 uM flufenamic acid-mediated inhibition of metabolite formation LC-MS/MS/FSA method
Drug metabolism in human liver cytosol treated with 20 uM [14C]SCH 534129 assessed as 100 uM diazepam-mediated inhibition of metabolite formation LC-MS/MS/FSA method
Drug metabolism in human liver cytosol treated with 20 uM [14C]SCH 534129 assessed as 1 mM ibuprofen-mediated inhibition of metabolite formation LC-MS/MS/FSA method
Drug metabolism in human liver cytosol treated with 20 uM [14C]SCH 534128 assessed as 1 mM BNPP-mediated inhibition of metabolite formation LC-MS/MS/FSA method
Drug metabolism in human liver cytosol treated with 20 uM [14C]SCH 534129 assessed as 1 mM BNPP-mediated inhibition of metabolite formation LC-MS/MS/FSA method