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Table 5 Maximum levels of inhibition of human and monkey plasma DPP activity using ala-pro-AFC as substrate

From: Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

  Rhesus Cyno Human
  IC50 (nM) Max % inhib IC50 (nM) Max % inhib IC50 (nM) Max % inhib
saxagliptin 2.9 ± 0.3 86 ± 1††† 2.4 ± 0.2 81 ± 6†† 4.0 ± 0.8 100 ± 0
vildagliptin 17 ± 5** 85 ± 1††† 13 ± 4** 79 ± 6†† 20 ± 7* 98 ± 1
sitagliptin 17 ± 2*** 87 ± 1††† 17 ± 2*** 80 ± 7†† 22 ± 3*** 98 ± 0
  1. N = 3 independent experiments. *P < 0.05, **P < 0.01, ***P < 0.001 versus saxagliptin. ††P < 0.01, †††P < 0.001 versus human