TABLE 5

Inhibitor constants for diclofenac and probenecid inhibition of 4MU glucuronidation by UGT isoforms a

Isoform
Ki b
Diclofenac
Probenecid
μM
1A1 52 ± 2 221 ± 1
1A6 60 ± 0.1 2790 ± 200
1A7 19 ± 2 96 ± 8
1A9 11 ± 1 2452 ± 101
1A10
28 ± 1
231 ± 13

  • ↵ a Competitive inhibition, except for inhibition of diclofenac (competitive-noncompetitive) and probenecid (noncompetitive) by UGT1A6.

  • ↵ b Ki ± standard error of fit.