Inhibition of human plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Inhibition of cynomolgus monkey plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Inhibition of recombinant mouse C-terminal 6His-tagged plasma kallikrein (20 to 638 residues) using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Inhibition of recombinant Sprague-Dawley rat plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Inhibition of rabbit plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Inhibition of pig plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Inhibition of dog plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
Drug metabolism in rat plasma assessed as (5R,8S,11S,14S,17S,20S,23R)-29-[[(2R)-2-acetamido-3-hydroxy-3-oxo-propyl]sulfanylmethyl]-5-amino-14-(3-amino-3-oxo-propyl)-17-(carboxymethyl)-11-(1H-imidazol-5-ylmethyl)-8,20-diisobutyl-6,9,12,15,18,21-hexaoxo-3,25-dithia-7,10,13,16,19,22-hexazabicyclo[25.3.1]hentriaconta-1(31),27,29-triene-23-carboxylic acid metabolite formation at 50 uM after 18 hrs by MALDI-TOF analysis
Drug metabolism in rat plasma assessed as (5R,8S,11S,14S,17S,20S,23R)-29-[[(2R)-2-acetamido-3-[[(1S)-2-hydroxy-1-(hydroxymethyl)-2-oxo-ethyl]amino]-3-oxo-propyl]sulfanylmethyl]-5-amino-14-(3-amino-3-oxo-propyl)-17-(carboxymethyl)-11-(1H-imidazol-5-ylmethyl)-8,20-diisobutyl-6,9,12,15,18,21-hexaoxo-3,25-dithia-7,10,13,16,19,22-hexazabicyclo[25.3.1]hentriaconta-1(31),27,29-triene-23-carboxylic acid metabolite formation at 50 uM after 18 hrs by MALDI-TOF analysis
Antiinflammatory activity in Sprague-Dawley rat carrageenan-induced paw edema model assessed as inhibition of paw edema AUC (0 to 2 hrs) at 10 to 30 mg/kg, ip pretreated for 15 mins followed by carrageenan challenge
Drug metabolism in rat plasma assessed as (5R,8S,11S,14S,17S,20S,23R)-29-[[(2R)-2-acetamido-3-[[(1S)-1-(hydroxymethyl)-2-[[(1S)-2-[(2S)-2-[[(1S)-2-hydroxy-1-methyl-2-oxo-ethyl]carbamoyl]pyrrolidin-1-yl]-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]amino]-2-oxo-ethyl]amino]-3-oxo-propyl]sulfanylmethyl]-5-amino-14-(3-amino-3-oxo-propyl)-17-(carboxymethyl)-11-(1H-imidazol-5-ylmethyl)-8,20-diisobutyl-6,9,12,15,18,21-hexaoxo-3,25-dithia-7,10,13,16,19,22-hexazabicyclo[25.3.1]hentriaconta-1(31),27,29-triene-23-carboxylic acid metabolite formation at 50 uM after 18 hrs by MALDI-TOF analysis