Skip to main content

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)