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Table 2 Inhibition of isolated, cloned human 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

1.3 ± 0.3 (12)

508 ± 174 (13)

98 ± 44 (11)

5-hydroxysaxagliptin

2.6 ± 1.0 (12)***

2495 ± 727 (14)*

423 ± 64 (12)

Vildagliptin

13 ± 2.8 (12)***

5218 ± 2319 (14)***

258 ± 93 (12)

Sitagliptin

18 ± 1.6 (12)***

33780 ± 5532 (12)***

55142 ± 19414 (11)***

  1. mean ± standard deviation (number of independent experiments). *P < 0.05, **P < 0.01, ***P < 0.001 versus saxagliptin
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BMC Pharmacology

ISSN: 1471-2210