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Table 1 Inhibition of isolated cloned human DPP4 at room temperature

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

compound

GLP-1 Ki (nM)

gly-pro-pNA Ki (nM)

Saxagliptin

0.41 ± 0.1 (7)

0.45 ± 0.1 (5)

Sitagliptin

2.5 ± 0.7 (4) ***

8 ± 1 (5)***

Vildagliptin

1.5 ± 0.5 (4) ***

7 ± 2 (5)***

  1. mean ± standard deviation (number of independent experiments). ***P < 0.001 versus saxagliptin