In Vitro Enzyme Inhibition Experiment

Inhibition of UGT by Nicardipine in HIM (Screening)

Inhibition was detected.  Cutoff used — 50% inhibition vs. control

4-methylumbelliferone

nicardipine 1318137

4-methylumbelliferone glucuronide

  • UGT

Cell fraction Individual human intestinal microsomes -7999704

Nicardipine was used as the positive control inhibitor.

Results

Percent inhibition was estimated from Fig. S1.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Purified green tea catechins were tested as inhibitors of UGT enzymes as described in Gufford et al., 2014 (Drug Metab Dispos. 2014 Oct;42(10):1675-83); information regarding incubation volume, time, and protien linearity were obtain therein.
Bovine serum albumin (0.05%) was added into the incubation system.

0.2 mg/mL

Commercially available

1410074

150 µL

20 min

UDPGA

Available

Not available

100 µM

400 µM