Table 2

Rates of RG 12525 N2-glucuronidation for microsome samples and expressed UGTs

Microsome Sample or Expressed UGT2-aRate of RG 12525N2-Glucuronide Formation
nmol/min/mg protein
Human intestine 010.043
Human intestine 020.052
UGT1A10.109
UGT1A30.125
UGT2B70.043

Expressed UGT forms (0.3 mg of protein per incubation) were assayed using 200 μM RG 12525 as described under Materials and Methods. The rate of N1-glucuronide formation was below the limit of quantitation in all samples.

  • 2-a  Expressed UGTs were supplied by Panvera Corporation. UGT1A1 from GENTEST Corp. showed comparatively lower activity.