Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay
Antidiabetic activity in Sprague-Dawley rat assessed as inhibition of blood glucose AUC at 3 mg/kg, po treated prior to dextrose challenge and measured after 20 to 60 mins by IPGTT relative to control
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay relative to AM-1638
Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 60 mins in presence of 100% human serum by HTRF assay relative to AM-1638
Agonist activity at recombinant rat GPR40 expressed in CHOK1 cells assessed as increase in IP1 accumulation measured after 60 mins by HTRF assay relative to AM-1638
Antidiabetic activity in po dosed Goto Kakizaki rats assessed as reduction in blood glucose excursion pretreated for 1 hr followed by dextrose challenge measured after 20 to 60 mins by OGTT method
Antidiabetic activity in po dosed Goto Kakizaki rats assessed as plasma concentration required for reduction in blood glucose excursion at MED pretreated for 1 hr followed by dextrose challenge measured 3 hrs post dose by OGTT
Inhibition of human BSEP expressed in baculovirus infected Sf9 insect cell membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholic acid uptake