Metabolic stability in ICR mouse liver microsomes assessed as parent compound remaining at 0.1 uM incubated for 60 mins in presence of NADPH by LC-MS/MS analysis
Inhibition of human recombinant DPP9 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay
Inhibition of human recombinant DPP8 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay
Inhibition of human recombinant DPP4 using Gly-Pro-AMC as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by fluorescence based microplate reader assay
In vivo inhibition of DPP4 in Sprague-Dawley rat plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 30 mins relative to control
In vivo inhibition of DPP4 in Sprague-Dawley rat plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 12 hrs relative to control
In vivo inhibition of DPP4 in Sprague-Dawley rat plasma at 10 mg/kg, po via gavage using Gly-Pro-AMC as substrate measured after 24 hrs relative to control
Hypoglycemic activity in ICR mouse assessed as reduction in glucose secretion at 10 mg/kg, po via gavage administered as single dose pretreated with compound followed by glucose challenge measured after 120 mins relative to control
Hypoglycemic activity in po dosed overnight fasted C57BL/6 db/db mouse assessed as improvement in glucose tolerance pretreated with compound for 30 mins followed by oral glucose challenge and measured up to 120 mins by glucometer