Inhibition of UGT1A1, 1A8, and 1A10 by Nicardipine (Positive Control; Screening) CSV JSON

In Vitro Enzyme Inhibition Experiment

Inhibition of UGT1A1, 1A8, and 1A10 by Nicardipine (Positive Control; Screening)

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

raloxifene 1513103

nicardipine 1318137

raloxifene 4'-glucuronide

  • UGT1A1 40782950
  • UGT1A10
  • UGT1A8

Cell fraction Pooled human intestinal microsomes -7999663

Information regarding enzymes involved in the formation of raloxifene metabolites was obtained from Gufford et al., 2015 (Drug Metab Dispos. 2015 Sep;43(9):1353-9).

Results

Percent inhibition was estimated from Fig. S2.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Commercially available

1410074

UDPGA

Not available

Not available

400 ┬ÁM