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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
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BMC Pharmacology

ISSN: 1471-2210