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Table 3 Inhibition of isolated, cloned cynomolgus monkey DPP4, DPP8 and DPP9 at 37°C

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

  DPP4 Ki (nM) DPP8 Ki (nM) DPP9 Ki (nM)
Saxagliptin 1.1 ± 0.2 (14) 390 ± 82 (6) 61 ± 5 (6)
5-hydroxysaxagliptin 2.9 ± 1.1 (13)*** 2061 ± 658 (6)*** 323 ± 60 (6)*
Vildagliptin 6.8 ± 2.0 (14)*** 3692 ± 917 (7)*** 125 ± 39 (7)***
Sitagliptin 15.6 ± 3.6 (14)*** 21949 ± 17461 (6)*** 65757 ± 7966 (6)***
  1. mean ± standard deviation (number of independent experiments). *P < 0.05, **P < 0.01, ***P < 0.001 versus saxagliptin