Prodrug activation in PBS/5% DMSO solution assessed as 3-(2,4-dihydroxyphenyl)-1-(2,5-dihydroxyphenyl)propan-1-one formation at 25 degC after 5 hrs by HPLC analysis
Prodrug conversion assessed as human recombinant CD26-mediated 3-(2,4-dihydroxyphenyl)-1-(2,5-dihydroxyphenyl)propan-1-one formation after 15 min by HPLC analysis
Prodrug conversion assessed as human recombinant CD26-mediated 3-(2,4-dihydroxyphenyl)-1-(2,5-dihydroxyphenyl)propan-1-one formation after 1 hr by HPLC analysis
Prodrug conversion in 20% human serum assessed as CD26-mediated 3-(2,4-dihydroxyphenyl)-1-(2,5-dihydroxyphenyl)propan-1-one formation after 60 mins by HPLC analysis
Prodrug conversion in 20% bovine serum assessed as CD26-mediated 3-(2,4-dihydroxyphenyl)-1-(2,5-dihydroxyphenyl)propan-1-one formation after 6 hrs by HPLC analysis
Positive allosteric modulation of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as acetyl choline-evoked currents at 10 uM at -80 mV holding potential prtreated for 2 mins followed by co-treatment with acetyl choline by electrophysiology method relative to acetyl choline