Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from human recombinant NPC1L1 expressed in HEK293 cells
Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from NPC1L1 in human enterocyte brush border membrane
Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from human intestinal brush border membrane NPC1L1 by single tube filtration assay
Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from recombinant human NPC1L1 expressed in HEK cells by single tube filtration assay
Displacement of [35S](2S,3S,4S,5R,6S)-6-(4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-1-(4-(3-(methylsulfonamido)prop-1-ynyl)phenyl)-4-oxoazetidin-2-yl)phenoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic acid from human NCP1L1 expressed in HEK 293
Binding affinity to FLAG/tGFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as localization at 10 uM after 24 hrs by fluorescence microscopy
Binding affinity to FLAG/tGFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as localization after 24 hrs by fluorescence microscopy
Binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to plasma membrane at 30 uM after 24 hrs by fluorescence microscopic analysis
Binding affinity to human EGFP-tagged NTD-deleted NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to plasma membrane after 24 hrs by fluorescence microscopic analysis
Binding affinity to human EGFP-tagged full-length NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as protein stabilization after 24 hrs by fluorescence assay
Binding affinity to human EGFP-tagged NTD-deleted NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as protein stabilization after 24 hrs by fluorescence assay
Binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to plasma membrane at 10 uM after 24 hrs by fluorescence microscopic analysis
Inhibition of NPC1L1 in human Caco2 cells assessed as decrease in cholesterol uptake at 100 uM preincubated for 24 hrs followed by stigmosterol substrate addition measured after 24 hrs by HPLC method relative to control
Inhibition of NPC1L1 in human Caco2 cells assessed as decrease in cholesterol uptake at 100 uM preincubated for 24 hrs followed by stigmosterol substrate addition measured after 24 hrs by HPLC method