Metabolic clearance (ul.min.nmol-1 CYP) of aliskiren hemifumarate for CYP4F3B was determined in human liver microsome incubated with [14C]SPP100 hemifumarate
Drug metabolism assessed as human CYP4F3A-mediated compound formation from 5 uM [14C]boceprevir after 120 mins by LC-MS/FSA method relative to total [14C]boceprevir
Activity at human recombinant CYP4F3A expressed in baculovirus-infected BTI-TN-5B1-4 insect cell microsomes assessed as metabolite formation at 5 to 100 M after 30 mins by HPLC-RA analysis
Activity at human recombinant CYP4F3B expressed in baculovirus-infected BTI-TN-5B1-4 insect cell microsomes assessed as relative abundance of compound formation treated with [14C]fingolimod at 100 uM after 30 mins by HPLC-RA analysis
Activity of human recombinant CYP4F3B assessed as enzyme-mediated drug metabolism treated with 25 uM vorapaxar after 120 mins by LC-MS/MS analysis in presence of NADPH
Activity of human recombinant CYP4F3A assessed as enzyme-mediated drug metabolism treated with 25 uM vorapaxar after 120 mins by LC-MS/MS analysis in presence of NADPH
Activity of human recombinant CYP4F3A assessed as enzyme-mediated (3R,3aS,4S,4aR,7R,8aR,9aR)-7-amino-4-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-3-methyldecahydronaphtho[2,3-c]furan-1(3H)-one formation at 25 uM after 120 mins by LC-MS/MS analysis in presence of NADPH
Drug level assessed as human recombinant CYP4F3A-mediated drug metabolism treated with 25 uM [14C]vorapaxar after 120 mins by LC-MS/MS analysis in presence of NADPH
Activity of human recombinant CYP4F3A assessed as enzyme-mediated 2-hydroxyethyl (1R,3aR,4aR,6R,8aR,9S,9aS)-9-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-ylcarbamate formation at 25 uM after 120 mins by LC-MS/MS analysis in presence of NADPH
Activity of human recombinant CYP4F3B assessed as enzyme-mediated 2-hydroxyethyl (1R,3aR,4aR,6R,8aR,9S,9aS)-9-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-ylcarbamate formation at 25 uM after 120 mins by LC-MS/MS analysis in presence of NADPH
Substrate activity at recombinant human CYP4F3B expressed in bactosomes assessed as CYP4F3B-mediated benzoic acid (6R,7S)-2,6,10-trihydroxy-1,3,11,12-tetramethoxy-6,7-dimethyl-5,6,7,8-tetrahydro-dibenzo[a,c]cycloocten-5-yl ester formation at 5 to 50 uM after 30 mins in presence of NADPH by UFLC-DAD analysis
Inhibition of recombinant human CYP4F3A expressed in baculovirus infected insect cells at 30 uM using Luc-4F2/3 as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo luciferase based luminescence assay
Inhibition of recombinant human CYP4F3B expressed in baculovirus infected insect cells at 30 uM using Luc-4F2/3 as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo luciferase based luminescence assay
Inhibition of recombinant human CYP4F3A expressed in baculovirus infected insect cells using Luc-4F2/3 as substrate after 10 mins in presence of NADPH by P450-glo luciferase based luminescence assay
Inhibition of recombinant human CYP4F3B expressed in baculovirus infected insect cells using Luc-4F2/3 as substrate after 10 mins in presence of NADPH by P450-glo luciferase based luminescence assay
Inhibition of recombinant human CYP4F3A expressed in baculovirus infected insect cells using Luc-4F2/3 as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo luciferase based luminescence assay
Inhibition of recombinant human CYP4F3B expressed in baculovirus infected insect cells using Luc-4F2/3 as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo luciferase based luminescence assay
Ratio of IC50 for inhibition of recombinant human CYP4F3A expressed in baculovirus infected insect cells using Luc-4F2/3 as substrate after 10 mins in presence of NADPH to IC50 for inhibition of recombinant human CYP4F3A expressed in baculovirus infected insect cells using Luc-4F2/3 as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo luciferase based luminescence assay