Inhibition of human SGLT1 expressed in CHOK1 cells assessed as reduction in sodium-dependent glucose uptake after 30 mins in presence of [14C]-methyl-alpha -D-glucopyranoside by microbeta counting method
Inhibition of human SGLT2 expressed in CHOK1 cells assessed as reduction in sodium-dependent glucose uptake after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by microbeta counting method
Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC (0 to 2 hrs) at 0.3 mg/kg, po dosed just prior to sucrose loading measured up to 120 mins by sucrose tolerance test relative to control
Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC (0 to 2 hrs) at 1 mg/kg, po dosed just prior to sucrose loading measured up to 120 mins by sucrose tolerance test relative to control
Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC (0 to 2 hrs) at 3 mg/kg, po dosed just prior to sucrose loading measured up to 120 mins by sucrose tolerance test relative to control
Drug uptake in Sprague-Dawley rat kidney assessed as unchanged drug level at 0.3 mg/kg, iv administered as single dose after 72 hrs by LCMS analysis relative to control
Antidiabetic activity in Sprague-Dawley rat assessed as reduction in blood glucose AUC (0 to 2 hrs) at 0.3 to 3 mg/kg, po dosed just prior to sucrose loading measured up to 120 mins by sucrose tolerance test relative to control
Gastrointestinal toxicity in Sprague-Dawley rat assessed as induction of diarrhea at 0.3 to 3 mg/kg, po dosed just prior to sucrose loading measured up to 120 mins during sucrose tolerance test relative to control