Competitive inhibition of His-tagged FimH carbohydrate recognizing domain expressed in Escherichia coli HM125 using ABTS-substrate after 3 hrs by calorimetric assay
Antagonist activity at Escherichia coli UT189 FimH in guinea pig red blood cells assessed as disaggregation of bacteria after 600 secs by aggregometry assay
Metabolic stability of the compound in mouse liver microsomes assessed as Cyp 450-mediated degradation at 2 uM after 30 mins by LC-MS analysis in presence of CES inhibitor BNPP
AUC (0 to 24 hrs) in plasma of urinary tract infection C3H/HeN mouse model at 50 mg/kg, iv administered as single dose measured after 6 hrs by LC-MS analysis
AUC (0 to 24 hrs) in urine of urinary tract infection C3H/HeN mouse model at 50 mg/kg, iv administered as single dose measured after 6 hrs by LC-MS analysis
Antibacterial activity against Escherichia coli UT189 infected in urinary tract infection C3H/HeN mouse model assessed as log reduction in bacterial CFU in urine of mouse at 50 mg/kg, iv administered as single dose 1 hr before infection and measured after 3 hrs post infection
Antibacterial activity against Escherichia coli UT189 infected in urinary tract infection C3H/HeN mouse model assessed as log reduction in bacterial CFU in bladder of mouse at 50 mg/kg, iv administered as single dose 1 hr before infection and measured after 3 hrs post infection
Antibacterial activity against Escherichia coli UT189 infected in urinary tract infection C3H/HeN mouse model assessed as reduction in bacterial count in kidney of mouse at 50 mg/kg, po administered as single dose 1 hr before infection and measured after 3 hrs post infection