5-Hydroxytryptophol-O-glucuronide (UGT1A6) is an authentic glucuronide standard and probe metabolite. 5-Hydroxytryptophol-O-glucuronide is used to detect the activity of human UGT1A6 in in vitro systems including human liver microsomes and recombinant UGT1A6 [1].
In Vitro, 5-Hydroxytryptophol-O-glucuronide (0.025 mg/mL HLM protein; 20-10000 µM 5HTOL; 20 min) formation via UGT1A6 in pooled human liver microsomes exhibits weak substrate inhibition kinetics with a mean Km of 420 µM without 2% BSA and 330 µM with 2% BSA, and minimal changes in unbound intrinsic clearance with BSA addition[1]. 5-Hydroxytryptophol-O-glucuronide (0.025 mg/mL rUGT1A6 protein; 20-10000 µM 5HTOL; 90 min) formation via recombinant UGT1A6 exhibits weak substrate inhibition kinetics with a mean Km of 570 µM without 2% BSA and 490 µM with 2% BSA, and a small increase in intrinsic clearance with BSA addition[1].
References:
[1]. Walsky RL, et al. Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors. Drug Metab Dispos. 2012;40(5):1051-1065.
In Vitro, 5-Hydroxytryptophol-O-glucuronide (0.025 mg/mL HLM protein; 20-10000 µM 5HTOL; 20 min) formation via UGT1A6 in pooled human liver microsomes exhibits weak substrate inhibition kinetics with a mean Km of 420 µM without 2% BSA and 330 µM with 2% BSA, and minimal changes in unbound intrinsic clearance with BSA addition[1]. 5-Hydroxytryptophol-O-glucuronide (0.025 mg/mL rUGT1A6 protein; 20-10000 µM 5HTOL; 90 min) formation via recombinant UGT1A6 exhibits weak substrate inhibition kinetics with a mean Km of 570 µM without 2% BSA and 490 µM with 2% BSA, and a small increase in intrinsic clearance with BSA addition[1].
References:
[1]. Walsky RL, et al. Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors. Drug Metab Dispos. 2012;40(5):1051-1065.