5-Hydroxytryptophol-O-glucuronide

5-Hydroxytryptophol-O-glucuronide is an authentic glucuronide standard and probe metabolite. It is utilized to assess the activity of human UGT1A6 in in vitro systems such as human liver microsomes and recombinant UGT1A6.

5-Hydroxytryptophol-O-glucuronide, at a concentration of 0.025 mg/mL HLM protein with 20-10000 µM 5HTOL over 20 minutes, exhibits weak substrate inhibition kinetics mediated by UGT1A6 in pooled human liver microsomes. The average K m is 420 µM without 2% BSA, and 330 µM with BSA addition, showing minimal change in intrinsic clearance when BSA is added. In a similar study with 0.025 mg/mL rUGT1A6 protein and 20-10000 µM 5HTOL over 90 minutes, formation mediated by recombinant UGT1A6 also demonstrates weak substrate inhibition kinetics. The K m averages 570 µM without 2% BSA and 490 µM with BSA, with a slight increase in intrinsic clearance upon BSA addition.