Prodrug activation assessed as human PSA mediated 4-((S)-2-((S)-2-Amino-3-hydroxypropanamido)-4-methylpentanamido)benzyl(R)-1-(((2R,3R,11bS)-3-ethyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl)methyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate formation by HPLC-MS analysis
Prodrug activation assessed as human PSA mediated 4-((S)-2-((S)-2-Amino-3-hydroxypropanamido)-4-methylpentanamido)benzyl(R)-1-(((2R,3R,11bS)-3-ethyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl)methyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate formation at 200 uM after 2 hrs by HPLC-MS analysis relative to control
Prodrug activation assessed as human PSA mediated 4-((S)-2-((S)-2-Amino-3-hydroxypropanamido)-4-methylpentanamido)benzyl(R)-1-(((2R,3R,11bS)-3-ethyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl)methyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate formation at 200 uM after 6 hrs by HPLC-MS analysis relative to control
Prodrug activation assessed as human PSA mediated 4-((S)-2-((S)-2-Amino-3-hydroxypropanamido)-4-methylpentanamido)benzyl(R)-1-(((2R,3R,11bS)-3-ethyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl)methyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate formation at 200 uM after 20 hrs by HPLC-MS analysis relative to control
Prodrug activation in human plasma assessed as human PSA mediated 4-((S)-2-((S)-2-Amino-3-hydroxypropanamido)-4-methylpentanamido)benzyl(R)-1-(((2R,3R,11bS)-3-ethyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl)methyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxylate formation at 200 uM after 48 hrs by HPLC-MS analysis