Inhibition of human recombinant C-terminal FLAG-tagged SMS2 expressed in Freestyle293 cell membrane using C14-phosphatidylcholineD72 and C17-ceramide pre-incubated for 60 mins followed by incubation with substrate for 30 mins measured by RapidFire/MS assay
Inhibition of mouse recombinant C-terminal FLAG-tagged SMS2 expressed in mammalian expression system using C14-phosphatidylcholineD72 and C17-ceramide pre-incubated for 60 mins followed by incubation with substrate for 30 mins measured by RapidFire/MS assay
Inhibition of human recombinant C-terminal FLAG-tagged SMS1 expressed in mammalian expression system using C14-phosphatidylcholineD72 and C17-ceramide pre-incubated for 60 mins followed by incubation with substrate for 30 mins measured by RapidFire/MS assay
In vivo inhibition of SMS2 in KK-AY/Ta mouse assessed as decrease in hepatic SM (22:00) levels at 100 mg/kg, sc qd for 7 days measured after last dosing by LC/MS analysis
In vivo inhibition of SMS2 in KK-AY/Ta mouse assessed as decrease in hepatic SM (22:00) levels at 200 mg/kg, sc bid for 7 days measured after last dosing by LC/MS analysis
In vivo inhibition of SMS2 in KK-AY/Ta mouse assessed as decrease in hepatic SM (22:00) levels at 100 mg/kg, po qd for 7 days measured after last dosing by LC/MS analysis
In vivo inhibition of SMS2 in KK-AY/Ta mouse assessed as decrease in hepatic SM (22:00) levels at 200 mg/kg, po bid for 7 days measured after last dosing by LC/MS analysis