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Table 2 Des-flurositagliptin dosed at ~400 mpk in feed is able to inhibit the DPP IV enzyme activity for 24 hours in blood.

From: Genetic ablation or pharmacological blockade of dipeptidyl peptidase IV does not impact T cell-dependent immune responses

 

Conversion of substrate in nmol/min

 

Day 1

Day 2

Day 3

Des-flurositagliptin, am bleed

4.53 ± 0.22

5.44 ± 0.79

6.12 ± 0.48

Des-flurositagliptin, pm bleed

4.90 ± 0.37

8.08 ± 1.8

8.29 ± 1.42

Control, am bleed

39.8 ± 4.0

47.5 ± 5.23

40.1 ± 6.94

Control, pm bleed

31.4 ± 0.65

43.3 ± 6.01

40.3 ± 7.65

DPP-IV-/- mice

1.02 ± 0.51

  
  1. The animals were fed chow milled with 6.7 grams of desflurositagliptin in 1 kg of Tekland chow to deliver an effective dose of 400 mpk. Blood were drawn 12 hours apart and DPP IV enzyme activity measured as described earlier. The animals (n = 4 in each group) were maintained on the inhibitor for the entire period of the experiment.