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Table 1 Percentage of glucuronide formation after exposure to liver species for 20 h (DAD at 240 nm) and selectivity for forming the glucuronide 3 sorted by increasing selectivity

From: Human UDP-glucuronosyltransferase UGT1A4 forms tertiary N-glucuronides predominately with the energetically less favored tautomer of substituted 1H-indazole (benzpyrazole)

Liver S9 homogenate from

2

3

Selectivity factor for 3 vs. 2

Rabbit

30.5%

6.7%

0.2

Mice

6.0%

4.9%

0.8

Dog

2.9%

2.8%

1

Chicken

4.4%

9.6%

2

Mini pig (miniature pig)

1.4%

6.4%

5

Horse

<0.1%

0.7%

8 a

Foal

<0.1%

1.4%

8 a

Porcine

1.6%

12.7%

8

Bovine

1.8%

24.0%

10

Rat

1.4%

26.9%

20

Sheep

0.4%

17.2%

45

Cynomolgus monkey

0.2%

13.4%

55

Guinea pig

0.2%

21.5%

101

Human

4.1%

77.1%

19

  1. aData from MS trace