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Table 4 On and off rates of DPP4 inhibitors 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

Compound

kon, 105 M-1 s-1

koff, 10-5 s-1

t1/2 (min.)

37°C

Saxagliptin

4.6 ± 0.6

23 ± 1

50

5-hydroxysaxagliptin

0.7 ± 0.1

50 ± 2

23

Vildagliptin

1.2 ± 0.2

330 ± 30

3.5

Sitagliptin

> 100

> 580

< 2

  1. mean ± standard error. Standard errors for kon were calculated from equations (2), (3) and (4), and for koff are from the fits to equation (5)
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BMC Pharmacology

ISSN: 1471-2210